Chemicals
Showing 36451–36600 of 41137 results
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SR 49059 is a selective, nonpeptide antagonist of the V1a subtype of the vasopressin receptor (Ki = 1.1-6.3 nM in human).{29120,14369} It demonstrates ≥2 orders of magnitude lower affinity for V1b, V2, and oxytocin receptors and does not exhibit any intrinsic agonist activity.{29120} SR 49059 can inhibit arginine vasopressin-induced human platelet aggregation with an IC50 value of 3.7 nM.{29120}
Brand:CaymanSKU:-Available on backorder
SR 49059 is a selective, nonpeptide antagonist of the V1a subtype of the vasopressin receptor (Ki = 1.1-6.3 nM in human).{29120,14369} It demonstrates ≥2 orders of magnitude lower affinity for V1b, V2, and oxytocin receptors and does not exhibit any intrinsic agonist activity.{29120} SR 49059 can inhibit arginine vasopressin-induced human platelet aggregation with an IC50 value of 3.7 nM.{29120}
Brand:CaymanSKU:-Available on backorder
SR 49059 is a selective, nonpeptide antagonist of the V1a subtype of the vasopressin receptor (Ki = 1.1-6.3 nM in human).{29120,14369} It demonstrates ≥2 orders of magnitude lower affinity for V1b, V2, and oxytocin receptors and does not exhibit any intrinsic agonist activity.{29120} SR 49059 can inhibit arginine vasopressin-induced human platelet aggregation with an IC50 value of 3.7 nM.{29120}
Brand:CaymanSKU:-Available on backorder
SR 49059 is a selective, nonpeptide antagonist of the V1a subtype of the vasopressin receptor (Ki = 1.1-6.3 nM in human).{29120,14369} It demonstrates ≥2 orders of magnitude lower affinity for V1b, V2, and oxytocin receptors and does not exhibit any intrinsic agonist activity.{29120} SR 49059 can inhibit arginine vasopressin-induced human platelet aggregation with an IC50 value of 3.7 nM.{29120}
Brand:CaymanSKU:-Available on backorder
SR 58611A is a selective β3-adrenergic receptor agonist (β3-AR; EC50 = 3.5 nM in rat colon).{38085} Its activity cannot be blocked by the β1- and β2-AR antagonists CGP 20712A and ICI 118551 (Item No. 15591), respectively. SR 58611A is minimally active against β1-ARs in rat uterus (EC50 = 499 nM) and inactive against β2-ARs in guinea pig trachea and atrium (EC50s = >10,000 and >30,000 nM, respectively). SR 58611A activates brown fat metabolism through activation of adenylyl cyclase activity and glycerol release in brown adipocytes (EC50s = 20 and 11 nM, respectively).{38086} It also reduces hypothermia produced by apomorphine (Item No. 16094) and reserpine (Item No. 16474) and potentiates toxicity produced by yohimbine (Item No. 19869) in mice.{38087} SR 58611A (0.6 to 2 mg/kg/day) also reduces the number of escape failures in a learned helplessness model of antidepressant-like activity in rats without changes in locomotor activity typically seen with β2-AR agonists.
Brand:CaymanSKU:11954 - 1 mgAvailable on backorder
SR 58611A is a selective β3-adrenergic receptor agonist (β3-AR; EC50 = 3.5 nM in rat colon).{38085} Its activity cannot be blocked by the β1- and β2-AR antagonists CGP 20712A and ICI 118551 (Item No. 15591), respectively. SR 58611A is minimally active against β1-ARs in rat uterus (EC50 = 499 nM) and inactive against β2-ARs in guinea pig trachea and atrium (EC50s = >10,000 and >30,000 nM, respectively). SR 58611A activates brown fat metabolism through activation of adenylyl cyclase activity and glycerol release in brown adipocytes (EC50s = 20 and 11 nM, respectively).{38086} It also reduces hypothermia produced by apomorphine (Item No. 16094) and reserpine (Item No. 16474) and potentiates toxicity produced by yohimbine (Item No. 19869) in mice.{38087} SR 58611A (0.6 to 2 mg/kg/day) also reduces the number of escape failures in a learned helplessness model of antidepressant-like activity in rats without changes in locomotor activity typically seen with β2-AR agonists.
Brand:CaymanSKU:11954 - 10 mgAvailable on backorder
SR 58611A is a selective β3-adrenergic receptor agonist (β3-AR; EC50 = 3.5 nM in rat colon).{38085} Its activity cannot be blocked by the β1- and β2-AR antagonists CGP 20712A and ICI 118551 (Item No. 15591), respectively. SR 58611A is minimally active against β1-ARs in rat uterus (EC50 = 499 nM) and inactive against β2-ARs in guinea pig trachea and atrium (EC50s = >10,000 and >30,000 nM, respectively). SR 58611A activates brown fat metabolism through activation of adenylyl cyclase activity and glycerol release in brown adipocytes (EC50s = 20 and 11 nM, respectively).{38086} It also reduces hypothermia produced by apomorphine (Item No. 16094) and reserpine (Item No. 16474) and potentiates toxicity produced by yohimbine (Item No. 19869) in mice.{38087} SR 58611A (0.6 to 2 mg/kg/day) also reduces the number of escape failures in a learned helplessness model of antidepressant-like activity in rats without changes in locomotor activity typically seen with β2-AR agonists.
Brand:CaymanSKU:11954 - 5 mgAvailable on backorder
SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively).{34206} It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively).{34205} At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism.{34203} In adipocytes, it induces phosphorylation of p38 MAPK via the Gs pathway.{34207} It has also been used in studies of heart failure to elucidate the role of the β3-ARs.{34204}
Brand:CaymanSKU:21407 -Out of stock
SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively).{34206} It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively).{34205} At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism.{34203} In adipocytes, it induces phosphorylation of p38 MAPK via the Gs pathway.{34207} It has also been used in studies of heart failure to elucidate the role of the β3-ARs.{34204}
Brand:CaymanSKU:21407 -Out of stock
SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively).{34206} It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively).{34205} At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism.{34203} In adipocytes, it induces phosphorylation of p38 MAPK via the Gs pathway.{34207} It has also been used in studies of heart failure to elucidate the role of the β3-ARs.{34204}
Brand:CaymanSKU:21407 -Out of stock
SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively).{34206} It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively).{34205} At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism.{34203} In adipocytes, it induces phosphorylation of p38 MAPK via the Gs pathway.{34207} It has also been used in studies of heart failure to elucidate the role of the β3-ARs.{34204}
Brand:CaymanSKU:21407 -Out of stock
SR 9186 is an inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 0.011 µM).{42411} It is highly selective for CYP3A4 over CYP3A5 (IC50 = 33 µM). SR 9186 inhibits metabolism of midazolam to 1’-hydroxy midazolam, testosterone to 6β-hydroxy testosterone, and vincristine to vincristine M1 in isolated human liver microsomes (HLMs) expressing recombinant CYP3A4 (IC50s = 9, 4, and 38 nM, respectively) but not microsomes expressing recombinant CYP3A5.{42412} It decreases lapatinib-induced quinoneimine-glutathione adduct formation in HLMs by 78% when used at a concentration of 2.5 µM.{42413}
Brand:CaymanSKU:-
SR 95531 is a derivative of γ-aminobutyric acid (GABA) that acts as an antagonist of GABAA receptors (Ki = 74-150 nM).{23068,23065,23067} When administered intravenously, it elicits seizures in mice.{23068} SR 95531 differs in action from bicuculline (Item No. 11727) in that it antagonizes GABA-induced chloride currents but not those induced by pentobarbitone.{23064} It is effective against GABAA receptor isoforms from mice, rats, and humans.{23068,23065,23063}
Brand:CaymanSKU:- SR 95531 is a derivative of γ-aminobutyric acid (GABA) that acts as an antagonist of GABAA receptors (Ki = 74-150 nM).{23068,23065,23067} When administered intravenously, it elicits seizures in mice.{23068} SR 95531 differs in action from bicuculline (Item No. 11727) in that it antagonizes GABA-induced chloride currents but not those induced by pentobarbitone.{23064} It is effective against GABAA receptor isoforms from mice, rats, and humans.{23068,23065,23063}
Brand:CaymanSKU:- SR 95531 is a derivative of γ-aminobutyric acid (GABA) that acts as an antagonist of GABAA receptors (Ki = 74-150 nM).{23068,23065,23067} When administered intravenously, it elicits seizures in mice.{23068} SR 95531 differs in action from bicuculline (Item No. 11727) in that it antagonizes GABA-induced chloride currents but not those induced by pentobarbitone.{23064} It is effective against GABAA receptor isoforms from mice, rats, and humans.{23068,23065,23063}
Brand:CaymanSKU:- SR 95531 is a derivative of γ-aminobutyric acid (GABA) that acts as an antagonist of GABAA receptors (Ki = 74-150 nM).{23068,23065,23067} When administered intravenously, it elicits seizures in mice.{23068} SR 95531 differs in action from bicuculline (Item No. 11727) in that it antagonizes GABA-induced chloride currents but not those induced by pentobarbitone.{23064} It is effective against GABAA receptor isoforms from mice, rats, and humans.{23068,23065,23063}
Brand:CaymanSKU:-
SR-12813 is a 1,1-bisphosphonate ester that exhibits hypocholesterolemic activity by enhancing the degradation of HMG-CoA reductase in various animal models.{30243} SR-12813 is also a high affinity ligand for human and rabbit pregnane X receptors (Kd = 41 nM; EC50 = 137 nM for hPXR in vitro) and can induce cytochrome P450 3A expression in human and rabbit hepatocytes.{30246,30245,30244}
Brand:CaymanSKU:-Available on backorder
SR-12813 is a 1,1-bisphosphonate ester that exhibits hypocholesterolemic activity by enhancing the degradation of HMG-CoA reductase in various animal models.{30243} SR-12813 is also a high affinity ligand for human and rabbit pregnane X receptors (Kd = 41 nM; EC50 = 137 nM for hPXR in vitro) and can induce cytochrome P450 3A expression in human and rabbit hepatocytes.{30246,30245,30244}
Brand:CaymanSKU:-Available on backorder
REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.{27845,21477} SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Item No. 11931).{21477} Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.{21477} SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.{27844}
Brand:CaymanSKU:-Out of stock
REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.{27845,21477} SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Item No. 11931).{21477} Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.{21477} SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.{27844}
Brand:CaymanSKU:-Out of stock
REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.{27845,21477} SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Item No. 11931).{21477} Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.{21477} SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.{27844}
Brand:CaymanSKU:-Out of stock
REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.{27845,21477} SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Item No. 11931).{21477} Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.{21477} SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.{27844}
Brand:CaymanSKU:-Out of stock
REV-ERBα and REV-ERBβ nuclear receptors are transcriptional repressors that coordinate circadian rhythm and metabolic pathways in a heme-dependent manner. SR9009 is a REV-ERB agonist that increases the constitutive repression of genes regulated by REV-ERBα and REV-ERBβ with IC50 values of 670 and 800 nM, respectively.{21074} Through activation of REV-ERB, SR9009 has been shown to decrease circadian locomotor activity during the dark phase and to alter the expression pattern of core clock genes in the hypothalami of mice.{21074} The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also shown to be altered in mice exposed to SR9009, resulting in increased energy expenditure.{21074} Diet-induced obese mice treated with 100 mg/kg SR9009 (i.p. two times a day for 30 days) have been reported to display decreased fat mass and markedly improved dyslipidemia and hyperglycemia.{21074}
Brand:CaymanSKU:11929 - 1 mgAvailable on backorder
REV-ERBα and REV-ERBβ nuclear receptors are transcriptional repressors that coordinate circadian rhythm and metabolic pathways in a heme-dependent manner. SR9009 is a REV-ERB agonist that increases the constitutive repression of genes regulated by REV-ERBα and REV-ERBβ with IC50 values of 670 and 800 nM, respectively.{21074} Through activation of REV-ERB, SR9009 has been shown to decrease circadian locomotor activity during the dark phase and to alter the expression pattern of core clock genes in the hypothalami of mice.{21074} The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also shown to be altered in mice exposed to SR9009, resulting in increased energy expenditure.{21074} Diet-induced obese mice treated with 100 mg/kg SR9009 (i.p. two times a day for 30 days) have been reported to display decreased fat mass and markedly improved dyslipidemia and hyperglycemia.{21074}
Brand:CaymanSKU:11929 - 10 mgAvailable on backorder
REV-ERBα and REV-ERBβ nuclear receptors are transcriptional repressors that coordinate circadian rhythm and metabolic pathways in a heme-dependent manner. SR9009 is a REV-ERB agonist that increases the constitutive repression of genes regulated by REV-ERBα and REV-ERBβ with IC50 values of 670 and 800 nM, respectively.{21074} Through activation of REV-ERB, SR9009 has been shown to decrease circadian locomotor activity during the dark phase and to alter the expression pattern of core clock genes in the hypothalami of mice.{21074} The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also shown to be altered in mice exposed to SR9009, resulting in increased energy expenditure.{21074} Diet-induced obese mice treated with 100 mg/kg SR9009 (i.p. two times a day for 30 days) have been reported to display decreased fat mass and markedly improved dyslipidemia and hyperglycemia.{21074}
Brand:CaymanSKU:11929 - 25 mgAvailable on backorder
REV-ERBα and REV-ERBβ nuclear receptors are transcriptional repressors that coordinate circadian rhythm and metabolic pathways in a heme-dependent manner. SR9009 is a REV-ERB agonist that increases the constitutive repression of genes regulated by REV-ERBα and REV-ERBβ with IC50 values of 670 and 800 nM, respectively.{21074} Through activation of REV-ERB, SR9009 has been shown to decrease circadian locomotor activity during the dark phase and to alter the expression pattern of core clock genes in the hypothalami of mice.{21074} The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also shown to be altered in mice exposed to SR9009, resulting in increased energy expenditure.{21074} Diet-induced obese mice treated with 100 mg/kg SR9009 (i.p. two times a day for 30 days) have been reported to display decreased fat mass and markedly improved dyslipidemia and hyperglycemia.{21074}
Brand:CaymanSKU:11929 - 5 mgAvailable on backorder
SR9011 is a REV-ERB agonist that increases the constitutive repression of genes regulated by REV-ERBα and REV-ERBβ with IC50 values of 790 and 560 nM, respectively.{21074} It has no activity at other nuclear receptors. SR9011 blocks the activity of the suprachiasmatic nucleus (SCN) clock, with reversible inhibition of circadian oscillation in SCN explants cultured from Per2-luc reporter mice.{21074} The circadian pattern of expression of several metabolic genes in liver, skeletal muscle, and adipose tissue was also shown to be altered in mice exposed to SR9011, resulting in increased energy expenditure.{21074}
Brand:CaymanSKU:11930 - 1 mgAvailable on backorder
SR9011 is a REV-ERB agonist that increases the constitutive repression of genes regulated by REV-ERBα and REV-ERBβ with IC50 values of 790 and 560 nM, respectively.{21074} It has no activity at other nuclear receptors. SR9011 blocks the activity of the suprachiasmatic nucleus (SCN) clock, with reversible inhibition of circadian oscillation in SCN explants cultured from Per2-luc reporter mice.{21074} The circadian pattern of expression of several metabolic genes in liver, skeletal muscle, and adipose tissue was also shown to be altered in mice exposed to SR9011, resulting in increased energy expenditure.{21074}
Brand:CaymanSKU:11930 - 5 mgAvailable on backorder
The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9238 is an inverse agonist of the two LXR isoforms, LXRα and LXRβ (IC50s = 214 and 43 nM, respectively).{30144} It displays liver specificity in vivo, with little action at peripheral LXR. SR9238 suppresses hepatic lipogenesis, inflammation, lipid accumulation, and fibrosis in mouse models of non-alcoholic steatohepatitis.{30144,30145} It also reduces plasma cholesterol levels in diet-induced obese mice.{30144}
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The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9238 is an inverse agonist of the two LXR isoforms, LXRα and LXRβ (IC50s = 214 and 43 nM, respectively).{30144} It displays liver specificity in vivo, with little action at peripheral LXR. SR9238 suppresses hepatic lipogenesis, inflammation, lipid accumulation, and fibrosis in mouse models of non-alcoholic steatohepatitis.{30144,30145} It also reduces plasma cholesterol levels in diet-induced obese mice.{30144}
Brand:CaymanSKU:-Available on backorder
The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9238 is an inverse agonist of the two LXR isoforms, LXRα and LXRβ (IC50s = 214 and 43 nM, respectively).{30144} It displays liver specificity in vivo, with little action at peripheral LXR. SR9238 suppresses hepatic lipogenesis, inflammation, lipid accumulation, and fibrosis in mouse models of non-alcoholic steatohepatitis.{30144,30145} It also reduces plasma cholesterol levels in diet-induced obese mice.{30144}
Brand:CaymanSKU:-Available on backorder
The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations.{29550} It reduces cancer cell viability (IC50 values range from 15 to 104 nM) without cytotoxicity against non-malignant cells.{29550} SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.{29550}
Brand:CaymanSKU:-Available on backorder
The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations.{29550} It reduces cancer cell viability (IC50 values range from 15 to 104 nM) without cytotoxicity against non-malignant cells.{29550} SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.{29550}
Brand:CaymanSKU:-Available on backorder
The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations.{29550} It reduces cancer cell viability (IC50 values range from 15 to 104 nM) without cytotoxicity against non-malignant cells.{29550} SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.{29550}
Brand:CaymanSKU:-Available on backorder
The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations.{29550} It reduces cancer cell viability (IC50 values range from 15 to 104 nM) without cytotoxicity against non-malignant cells.{29550} SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.{29550}
Brand:CaymanSKU:-Available on backorder
The Src kinases constitute a family of non-receptor tyrosine kinases, which includes Src and Lck. Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.{23054,17331} It less effectively blocks the receptor tyrosine kinases VEGFR2 and C-fms (IC50 = 0.32 and 30 µM), as well as a long list of serine/threonine kinases.{23054,17331} Src Kinase Inhibitor I also inhibits receptor-interacting protein-2 with an IC50 value of 26 nM.{17331}
Brand:CaymanSKU:- The Src kinases constitute a family of non-receptor tyrosine kinases, which includes Src and Lck. Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.{23054,17331} It less effectively blocks the receptor tyrosine kinases VEGFR2 and C-fms (IC50 = 0.32 and 30 µM), as well as a long list of serine/threonine kinases.{23054,17331} Src Kinase Inhibitor I also inhibits receptor-interacting protein-2 with an IC50 value of 26 nM.{17331}
Brand:CaymanSKU:- The Src kinases constitute a family of non-receptor tyrosine kinases, which includes Src and Lck. Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.{23054,17331} It less effectively blocks the receptor tyrosine kinases VEGFR2 and C-fms (IC50 = 0.32 and 30 µM), as well as a long list of serine/threonine kinases.{23054,17331} Src Kinase Inhibitor I also inhibits receptor-interacting protein-2 with an IC50 value of 26 nM.{17331}
Brand:CaymanSKU:- The Src kinases constitute a family of non-receptor tyrosine kinases, which includes Src and Lck. Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.{23054,17331} It less effectively blocks the receptor tyrosine kinases VEGFR2 and C-fms (IC50 = 0.32 and 30 µM), as well as a long list of serine/threonine kinases.{23054,17331} Src Kinase Inhibitor I also inhibits receptor-interacting protein-2 with an IC50 value of 26 nM.{17331}
Brand:CaymanSKU:-
SRI-011381 is an activator of TGF-β signaling.{47687} It reduces increases in cell death and the number of dystrophic neurites induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in primary mouse embryonic forebrain neurons when used at a concentration of 3 µM. SRI-011381 (2 and 5 µM) increases phagocytosis of Aβ42 by greater than 20% in J774A.1 and THP-1 macrophages. It increases contextual fear conditioning freezing time and spontaneous alternations in the Y-maze, indicating prevention of memory deficits, in the APP751Lon,Swe transgenic mouse model of Alzheimer’s disease when administered at a dose of 10 mg/kg for 10 weeks.
Brand:CaymanSKU:28914 - 1 mgAvailable on backorder
SRI-011381 is an activator of TGF-β signaling.{47687} It reduces increases in cell death and the number of dystrophic neurites induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in primary mouse embryonic forebrain neurons when used at a concentration of 3 µM. SRI-011381 (2 and 5 µM) increases phagocytosis of Aβ42 by greater than 20% in J774A.1 and THP-1 macrophages. It increases contextual fear conditioning freezing time and spontaneous alternations in the Y-maze, indicating prevention of memory deficits, in the APP751Lon,Swe transgenic mouse model of Alzheimer’s disease when administered at a dose of 10 mg/kg for 10 weeks.
Brand:CaymanSKU:28914 - 10 mgAvailable on backorder
SRI-011381 is an activator of TGF-β signaling.{47687} It reduces increases in cell death and the number of dystrophic neurites induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in primary mouse embryonic forebrain neurons when used at a concentration of 3 µM. SRI-011381 (2 and 5 µM) increases phagocytosis of Aβ42 by greater than 20% in J774A.1 and THP-1 macrophages. It increases contextual fear conditioning freezing time and spontaneous alternations in the Y-maze, indicating prevention of memory deficits, in the APP751Lon,Swe transgenic mouse model of Alzheimer’s disease when administered at a dose of 10 mg/kg for 10 weeks.
Brand:CaymanSKU:28914 - 5 mgAvailable on backorder
SRI-011381 is an activator of TGF-β signaling.{47687} It reduces increases in cell death and the number of dystrophic neurites induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in primary mouse embryonic forebrain neurons when used at a concentration of 3 µM. SRI-011381 (2 and 5 µM) increases phagocytosis of Aβ42 by greater than 20% in J774A.1 and THP-1 macrophages. It increases contextual fear conditioning freezing time and spontaneous alternations in the Y-maze, indicating prevention of memory deficits, in the APP751Lon,Swe transgenic mouse model of Alzheimer’s disease when administered at a dose of 10 mg/kg for 10 weeks.
Brand:CaymanSKU:28914 - 500 µgAvailable on backorder
Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1.{27537} SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (Ki = 0.89 µM).{27539} It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4.{27539} SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells.{27539,27538} By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.{27543,27541,27540}
Brand:CaymanSKU:- Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1.{27537} SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (Ki = 0.89 µM).{27539} It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4.{27539} SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells.{27539,27538} By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.{27543,27541,27540}
Brand:CaymanSKU:- Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1.{27537} SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (Ki = 0.89 µM).{27539} It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4.{27539} SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells.{27539,27538} By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.{27543,27541,27540}
Brand:CaymanSKU:- Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1.{27537} SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (Ki = 0.89 µM).{27539} It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4.{27539} SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells.{27539,27538} By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.{27543,27541,27540}
Brand:CaymanSKU:-
SRS11-92 is a ferroptosis inhibitor and a derivative of ferrostatin-1 (Item No. 17729).{28857} It inhibits ferroptotic cell death induced by erastin (Item No. 17754) in HT-1080 human fibrosarcoma cells (EC50 = 6 nM). SRS11-92 (2 µM) inhibits iron-induced cell death in isolated mouse kidney proximal tubules, and fully protects rat oligodendrocytes from cystine deprivation-induced cell death in an in vitro model of periventricular leukomalacia when used at a concentration of 100 nM. It also increases survival of medium spiny neurons in rat corticostriatal brain slices in an in vitro model of Huntington’s disease in a concentration-dependent manner. SRS11-92 (3 µM) increases production of reactive oxygen species (ROS) in L. major promastigotes in a time-dependent manner.{42388} It is selectively toxic to L. major promastigotes (LD50 = 3.34 µM) over U2OS human osteoblasts, RAW 264.7 macrophages, and intraperitoneal macrophages when used at a concentration of 80 µM.
Brand:CaymanSKU:25689 - 1 mgAvailable on backorder
SRS11-92 is a ferroptosis inhibitor and a derivative of ferrostatin-1 (Item No. 17729).{28857} It inhibits ferroptotic cell death induced by erastin (Item No. 17754) in HT-1080 human fibrosarcoma cells (EC50 = 6 nM). SRS11-92 (2 µM) inhibits iron-induced cell death in isolated mouse kidney proximal tubules, and fully protects rat oligodendrocytes from cystine deprivation-induced cell death in an in vitro model of periventricular leukomalacia when used at a concentration of 100 nM. It also increases survival of medium spiny neurons in rat corticostriatal brain slices in an in vitro model of Huntington’s disease in a concentration-dependent manner. SRS11-92 (3 µM) increases production of reactive oxygen species (ROS) in L. major promastigotes in a time-dependent manner.{42388} It is selectively toxic to L. major promastigotes (LD50 = 3.34 µM) over U2OS human osteoblasts, RAW 264.7 macrophages, and intraperitoneal macrophages when used at a concentration of 80 µM.
Brand:CaymanSKU:25689 - 10 mgAvailable on backorder
SRS11-92 is a ferroptosis inhibitor and a derivative of ferrostatin-1 (Item No. 17729).{28857} It inhibits ferroptotic cell death induced by erastin (Item No. 17754) in HT-1080 human fibrosarcoma cells (EC50 = 6 nM). SRS11-92 (2 µM) inhibits iron-induced cell death in isolated mouse kidney proximal tubules, and fully protects rat oligodendrocytes from cystine deprivation-induced cell death in an in vitro model of periventricular leukomalacia when used at a concentration of 100 nM. It also increases survival of medium spiny neurons in rat corticostriatal brain slices in an in vitro model of Huntington’s disease in a concentration-dependent manner. SRS11-92 (3 µM) increases production of reactive oxygen species (ROS) in L. major promastigotes in a time-dependent manner.{42388} It is selectively toxic to L. major promastigotes (LD50 = 3.34 µM) over U2OS human osteoblasts, RAW 264.7 macrophages, and intraperitoneal macrophages when used at a concentration of 80 µM.
Brand:CaymanSKU:25689 - 25 mgAvailable on backorder
SRS11-92 is a ferroptosis inhibitor and a derivative of ferrostatin-1 (Item No. 17729).{28857} It inhibits ferroptotic cell death induced by erastin (Item No. 17754) in HT-1080 human fibrosarcoma cells (EC50 = 6 nM). SRS11-92 (2 µM) inhibits iron-induced cell death in isolated mouse kidney proximal tubules, and fully protects rat oligodendrocytes from cystine deprivation-induced cell death in an in vitro model of periventricular leukomalacia when used at a concentration of 100 nM. It also increases survival of medium spiny neurons in rat corticostriatal brain slices in an in vitro model of Huntington’s disease in a concentration-dependent manner. SRS11-92 (3 µM) increases production of reactive oxygen species (ROS) in L. major promastigotes in a time-dependent manner.{42388} It is selectively toxic to L. major promastigotes (LD50 = 3.34 µM) over U2OS human osteoblasts, RAW 264.7 macrophages, and intraperitoneal macrophages when used at a concentration of 80 µM.
Brand:CaymanSKU:25689 - 5 mgAvailable on backorder
SRS16-86 is an inhibitor of ferroptosis.{43387} It inhibits ferroptosis induced by erastin (Item No. 17754) in HT-1080 and NIH3T3 cells when used at a concentration of 1 μM. SRS16-86 (2 mg/kg) prevents renal tubular damage and increases in serum levels of urea and creatine in a mouse model of renal ischemia-reperfusion injury (IRI). In a rat model of spinal cord injury, SRS16-86 (15 mg/kg) increases the levels of glutathione peroxidase 4 (GPX4), system xc- cystine/glutamate transporter (xCT), and glutathione (GSH) and decreases levels of IL-1β, TNF-α, ICAM-1, and the lipid peroxidation marker 4-hydroxy nonenal (4HNE) in injured spinal cord epicenters.{43841} It also increases tissue sparing and improves locomotor recovery in the same model.
Brand:CaymanSKU:26752 - 1 mgAvailable on backorder
SRS16-86 is an inhibitor of ferroptosis.{43387} It inhibits ferroptosis induced by erastin (Item No. 17754) in HT-1080 and NIH3T3 cells when used at a concentration of 1 μM. SRS16-86 (2 mg/kg) prevents renal tubular damage and increases in serum levels of urea and creatine in a mouse model of renal ischemia-reperfusion injury (IRI). In a rat model of spinal cord injury, SRS16-86 (15 mg/kg) increases the levels of glutathione peroxidase 4 (GPX4), system xc- cystine/glutamate transporter (xCT), and glutathione (GSH) and decreases levels of IL-1β, TNF-α, ICAM-1, and the lipid peroxidation marker 4-hydroxy nonenal (4HNE) in injured spinal cord epicenters.{43841} It also increases tissue sparing and improves locomotor recovery in the same model.
Brand:CaymanSKU:26752 - 5 mgAvailable on backorder
SRS16-86 is an inhibitor of ferroptosis.{43387} It inhibits ferroptosis induced by erastin (Item No. 17754) in HT-1080 and NIH3T3 cells when used at a concentration of 1 μM. SRS16-86 (2 mg/kg) prevents renal tubular damage and increases in serum levels of urea and creatine in a mouse model of renal ischemia-reperfusion injury (IRI). In a rat model of spinal cord injury, SRS16-86 (15 mg/kg) increases the levels of glutathione peroxidase 4 (GPX4), system xc- cystine/glutamate transporter (xCT), and glutathione (GSH) and decreases levels of IL-1β, TNF-α, ICAM-1, and the lipid peroxidation marker 4-hydroxy nonenal (4HNE) in injured spinal cord epicenters.{43841} It also increases tissue sparing and improves locomotor recovery in the same model.
Brand:CaymanSKU:26752 - 500 µgAvailable on backorder
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. SRT 1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively).{16225} In diet-induced obese and diabetic leptin-deficient ob/ob mice, oral administration of 100 mg/kg SRT1720 once daily improves insulin sensitivity, lowers plasma glucose and increases mitochondrial capacity after one week of treatment.{16225} In Zucker fa/fa rats, SRT 1720 improves whole-body glucose homeostasis and insulin sensitivity in adipose tissue, skeletal muscle, and liver.{16225}
Brand:CaymanSKU:10011020 - 1 mgAvailable on backorder
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. SRT 1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively).{16225} In diet-induced obese and diabetic leptin-deficient ob/ob mice, oral administration of 100 mg/kg SRT1720 once daily improves insulin sensitivity, lowers plasma glucose and increases mitochondrial capacity after one week of treatment.{16225} In Zucker fa/fa rats, SRT 1720 improves whole-body glucose homeostasis and insulin sensitivity in adipose tissue, skeletal muscle, and liver.{16225}
Brand:CaymanSKU:10011020 - 10 mgAvailable on backorder
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. SRT 1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively).{16225} In diet-induced obese and diabetic leptin-deficient ob/ob mice, oral administration of 100 mg/kg SRT1720 once daily improves insulin sensitivity, lowers plasma glucose and increases mitochondrial capacity after one week of treatment.{16225} In Zucker fa/fa rats, SRT 1720 improves whole-body glucose homeostasis and insulin sensitivity in adipose tissue, skeletal muscle, and liver.{16225}
Brand:CaymanSKU:10011020 - 5 mgAvailable on backorder
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. SRT 1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively).{16225} In diet-induced obese and diabetic leptin-deficient ob/ob mice, oral administration of 100 mg/kg SRT1720 once daily improves insulin sensitivity, lowers plasma glucose and increases mitochondrial capacity after one week of treatment.{16225} In Zucker fa/fa rats, SRT 1720 improves whole-body glucose homeostasis and insulin sensitivity in adipose tissue, skeletal muscle, and liver.{16225}
Brand:CaymanSKU:10011020 - 50 mgAvailable on backorder
SRT 2104 is an activator of sirtuin 1 (SIRT1).{42917} It increases renal SIRT1 activity and protein levels and decreases acetylation of the SIRT1 substrate p53 in a mouse model of diabetes induced by streptozotocin (STZ; Item No. 13104), as well as in non-diabetic control animals, when administered at a dose of approximately 100 mg/kg in the diet. SRT 2104 also decreases renal levels of inducible nitric oxide synthase (iNOS), reactive oxygen species (ROS), and malondialdehyde (MDA), as well as the fibrotic markers TGF-β1 and CTGF and the inflammatory markers PAI-1 and VCAM-1, in STZ-induced diabetic mice. SRT 2104 (0.5% in the diet) increases lifespan, improves motor function in the balance beam test, and reduces atrophy of the neocortex in the N171-82Q mouse model of Huntington’s disease.{42918}
Brand:CaymanSKU:28380 - 1 mgAvailable on backorder
SRT 2104 is an activator of sirtuin 1 (SIRT1).{42917} It increases renal SIRT1 activity and protein levels and decreases acetylation of the SIRT1 substrate p53 in a mouse model of diabetes induced by streptozotocin (STZ; Item No. 13104), as well as in non-diabetic control animals, when administered at a dose of approximately 100 mg/kg in the diet. SRT 2104 also decreases renal levels of inducible nitric oxide synthase (iNOS), reactive oxygen species (ROS), and malondialdehyde (MDA), as well as the fibrotic markers TGF-β1 and CTGF and the inflammatory markers PAI-1 and VCAM-1, in STZ-induced diabetic mice. SRT 2104 (0.5% in the diet) increases lifespan, improves motor function in the balance beam test, and reduces atrophy of the neocortex in the N171-82Q mouse model of Huntington’s disease.{42918}
Brand:CaymanSKU:28380 - 10 mgAvailable on backorder
SRT 2104 is an activator of sirtuin 1 (SIRT1).{42917} It increases renal SIRT1 activity and protein levels and decreases acetylation of the SIRT1 substrate p53 in a mouse model of diabetes induced by streptozotocin (STZ; Item No. 13104), as well as in non-diabetic control animals, when administered at a dose of approximately 100 mg/kg in the diet. SRT 2104 also decreases renal levels of inducible nitric oxide synthase (iNOS), reactive oxygen species (ROS), and malondialdehyde (MDA), as well as the fibrotic markers TGF-β1 and CTGF and the inflammatory markers PAI-1 and VCAM-1, in STZ-induced diabetic mice. SRT 2104 (0.5% in the diet) increases lifespan, improves motor function in the balance beam test, and reduces atrophy of the neocortex in the N171-82Q mouse model of Huntington’s disease.{42918}
Brand:CaymanSKU:28380 - 25 mgAvailable on backorder
SRT 2104 is an activator of sirtuin 1 (SIRT1).{42917} It increases renal SIRT1 activity and protein levels and decreases acetylation of the SIRT1 substrate p53 in a mouse model of diabetes induced by streptozotocin (STZ; Item No. 13104), as well as in non-diabetic control animals, when administered at a dose of approximately 100 mg/kg in the diet. SRT 2104 also decreases renal levels of inducible nitric oxide synthase (iNOS), reactive oxygen species (ROS), and malondialdehyde (MDA), as well as the fibrotic markers TGF-β1 and CTGF and the inflammatory markers PAI-1 and VCAM-1, in STZ-induced diabetic mice. SRT 2104 (0.5% in the diet) increases lifespan, improves motor function in the balance beam test, and reduces atrophy of the neocortex in the N171-82Q mouse model of Huntington’s disease.{42918}
Brand:CaymanSKU:28380 - 5 mgAvailable on backorder
SS-208 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 12 nM).{50457} It is selective for HDAC6 over HDAC1, -4, -5, -7, -8, -9, and -11 (IC50s = 1.39, 19.5, 6.91, 8.34, 1.23, 38.2, and 5.12 µM, respectively). SS-208 (0.1-25 µM) inhibits HDAC6 in, but does not induce cell death of, human PC3 prostate, 5637 and T24 bladder, and murine SM1 melanoma cells in vitro. It decreases protein levels of programmed death ligand 1 (PD-L1) in SM1 cells when used at a concentration of 5 µM. SS-208 (25 mg/kg, i.p.) reduces tumor growth and increases the number of intratumoral CD8+, CD4+, and natural killer (NK) T cells in an SM1 murine melanoma model.
Brand:CaymanSKU:29128 - 1 mgAvailable on backorder
SS-208 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 12 nM).{50457} It is selective for HDAC6 over HDAC1, -4, -5, -7, -8, -9, and -11 (IC50s = 1.39, 19.5, 6.91, 8.34, 1.23, 38.2, and 5.12 µM, respectively). SS-208 (0.1-25 µM) inhibits HDAC6 in, but does not induce cell death of, human PC3 prostate, 5637 and T24 bladder, and murine SM1 melanoma cells in vitro. It decreases protein levels of programmed death ligand 1 (PD-L1) in SM1 cells when used at a concentration of 5 µM. SS-208 (25 mg/kg, i.p.) reduces tumor growth and increases the number of intratumoral CD8+, CD4+, and natural killer (NK) T cells in an SM1 murine melanoma model.
Brand:CaymanSKU:29128 - 10 mgAvailable on backorder
SS-208 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 12 nM).{50457} It is selective for HDAC6 over HDAC1, -4, -5, -7, -8, -9, and -11 (IC50s = 1.39, 19.5, 6.91, 8.34, 1.23, 38.2, and 5.12 µM, respectively). SS-208 (0.1-25 µM) inhibits HDAC6 in, but does not induce cell death of, human PC3 prostate, 5637 and T24 bladder, and murine SM1 melanoma cells in vitro. It decreases protein levels of programmed death ligand 1 (PD-L1) in SM1 cells when used at a concentration of 5 µM. SS-208 (25 mg/kg, i.p.) reduces tumor growth and increases the number of intratumoral CD8+, CD4+, and natural killer (NK) T cells in an SM1 murine melanoma model.
Brand:CaymanSKU:29128 - 25 mgAvailable on backorder
SS-208 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 12 nM).{50457} It is selective for HDAC6 over HDAC1, -4, -5, -7, -8, -9, and -11 (IC50s = 1.39, 19.5, 6.91, 8.34, 1.23, 38.2, and 5.12 µM, respectively). SS-208 (0.1-25 µM) inhibits HDAC6 in, but does not induce cell death of, human PC3 prostate, 5637 and T24 bladder, and murine SM1 melanoma cells in vitro. It decreases protein levels of programmed death ligand 1 (PD-L1) in SM1 cells when used at a concentration of 5 µM. SS-208 (25 mg/kg, i.p.) reduces tumor growth and increases the number of intratumoral CD8+, CD4+, and natural killer (NK) T cells in an SM1 murine melanoma model.
Brand:CaymanSKU:29128 - 5 mgAvailable on backorder
SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.{58163} It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50 = 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50 = 5.33 µM) but not cathepsin B when used at a concentration of 20 µM.
Brand:CaymanSKU:32582 - 1 mgAvailable on backorder
SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.{58163} It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50 = 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50 = 5.33 µM) but not cathepsin B when used at a concentration of 20 µM.
Brand:CaymanSKU:32582 - 10 mgAvailable on backorder
SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.{58163} It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50 = 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50 = 5.33 µM) but not cathepsin B when used at a concentration of 20 µM.
Brand:CaymanSKU:32582 - 25 mgAvailable on backorder
SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.{58163} It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50 = 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50 = 5.33 µM) but not cathepsin B when used at a concentration of 20 µM.
Brand:CaymanSKU:32582 - 5 mgAvailable on backorder
SSR 128129E is a potent inhibitor of the FGF receptor (FGFR; IC50 = 1.9 nM).{42030} It reduces FGF2-induced endothelial cell proliferation and migration (IC50s = 31 and 15.2 nM, respectively), as well as lamellipodia formation in vitro. SSR 128129E also reduces proliferation of PAE cells expressing FGFR1, mPanc02 cells expressing FGFR2, hB9 myeloma cells expressing FGFR3, and HUVECs expressing FGFR4 when used at a concentration of 100 nM. In vivo, SSR 128129E (30 mg/kg per day) reduces limb swelling, redness, and deformity and improves performance in an exercise endurance test in a mouse model of arthritis. It reduces tumor growth and metastasis and enhances antitumor activity of the VEGF receptor (VEGFR) antibody αVEGFR2 in a Panc02 mouse orthotopic tumor model. SSR 128129E (50 mg/kg per day) reduces atherosclerotic lesion size in the aortic sinus of apoE-/- mice.{42031} It also reduces intimal hyperplasia following jugular vein-to-artery bypass grafting surgery in rats.{42032}
Brand:CaymanSKU:22128 -Out of stock
SSR 128129E is a potent inhibitor of the FGF receptor (FGFR; IC50 = 1.9 nM).{42030} It reduces FGF2-induced endothelial cell proliferation and migration (IC50s = 31 and 15.2 nM, respectively), as well as lamellipodia formation in vitro. SSR 128129E also reduces proliferation of PAE cells expressing FGFR1, mPanc02 cells expressing FGFR2, hB9 myeloma cells expressing FGFR3, and HUVECs expressing FGFR4 when used at a concentration of 100 nM. In vivo, SSR 128129E (30 mg/kg per day) reduces limb swelling, redness, and deformity and improves performance in an exercise endurance test in a mouse model of arthritis. It reduces tumor growth and metastasis and enhances antitumor activity of the VEGF receptor (VEGFR) antibody αVEGFR2 in a Panc02 mouse orthotopic tumor model. SSR 128129E (50 mg/kg per day) reduces atherosclerotic lesion size in the aortic sinus of apoE-/- mice.{42031} It also reduces intimal hyperplasia following jugular vein-to-artery bypass grafting surgery in rats.{42032}
Brand:CaymanSKU:22128 -Out of stock
SSR 128129E is a potent inhibitor of the FGF receptor (FGFR; IC50 = 1.9 nM).{42030} It reduces FGF2-induced endothelial cell proliferation and migration (IC50s = 31 and 15.2 nM, respectively), as well as lamellipodia formation in vitro. SSR 128129E also reduces proliferation of PAE cells expressing FGFR1, mPanc02 cells expressing FGFR2, hB9 myeloma cells expressing FGFR3, and HUVECs expressing FGFR4 when used at a concentration of 100 nM. In vivo, SSR 128129E (30 mg/kg per day) reduces limb swelling, redness, and deformity and improves performance in an exercise endurance test in a mouse model of arthritis. It reduces tumor growth and metastasis and enhances antitumor activity of the VEGF receptor (VEGFR) antibody αVEGFR2 in a Panc02 mouse orthotopic tumor model. SSR 128129E (50 mg/kg per day) reduces atherosclerotic lesion size in the aortic sinus of apoE-/- mice.{42031} It also reduces intimal hyperplasia following jugular vein-to-artery bypass grafting surgery in rats.{42032}
Brand:CaymanSKU:22128 -Out of stock
SSR 128129E is a potent inhibitor of the FGF receptor (FGFR; IC50 = 1.9 nM).{42030} It reduces FGF2-induced endothelial cell proliferation and migration (IC50s = 31 and 15.2 nM, respectively), as well as lamellipodia formation in vitro. SSR 128129E also reduces proliferation of PAE cells expressing FGFR1, mPanc02 cells expressing FGFR2, hB9 myeloma cells expressing FGFR3, and HUVECs expressing FGFR4 when used at a concentration of 100 nM. In vivo, SSR 128129E (30 mg/kg per day) reduces limb swelling, redness, and deformity and improves performance in an exercise endurance test in a mouse model of arthritis. It reduces tumor growth and metastasis and enhances antitumor activity of the VEGF receptor (VEGFR) antibody αVEGFR2 in a Panc02 mouse orthotopic tumor model. SSR 128129E (50 mg/kg per day) reduces atherosclerotic lesion size in the aortic sinus of apoE-/- mice.{42031} It also reduces intimal hyperplasia following jugular vein-to-artery bypass grafting surgery in rats.{42032}
Brand:CaymanSKU:22128 -Out of stock
SSR 240612 is a selective, non-peptide antagonist of the bradykinin B1 receptor (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).{45045} It inhibits the contraction of rabbit aorta and rat ileum induced by the B1 receptor agonist des-Arg9-bradykinin (des-Arg9-BK) ex vivo in a concentration-dependent manner. SSR 240612 (0.3 mg/kg) reduces tissue damage and neutrophil accumulation in a rat model of splanchnic artery occlusion/reperfusion-induced intestinal injury and inhibits des-Arg9-BK-induced paw edema in mice when administered orally at doses of 3 and 10 mg/kg or intraperitoneally at doses of 0.3 and 1 mg/kg. SSR 240612 (10 mg/kg per day) reduces fibrosis in a unilateral ureteral obstruction mouse model of kidney fibrosis.{45046} It also reduces mean arterial blood pressure in two rat models of hypertension when administered at doses of 5 and 10 mg/kg and reduces plasma glucose and insulin levels in a glucose-fed rat model of insulin resistance when administered at a dose of 10 mg/kg per day.{45047,45048} SSR 240612 also exhibits analgesic properties in several rodent models of hyperalgesia.{45045}
Brand:CaymanSKU:25544 - 1 mgAvailable on backorder
SSR 240612 is a selective, non-peptide antagonist of the bradykinin B1 receptor (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).{45045} It inhibits the contraction of rabbit aorta and rat ileum induced by the B1 receptor agonist des-Arg9-bradykinin (des-Arg9-BK) ex vivo in a concentration-dependent manner. SSR 240612 (0.3 mg/kg) reduces tissue damage and neutrophil accumulation in a rat model of splanchnic artery occlusion/reperfusion-induced intestinal injury and inhibits des-Arg9-BK-induced paw edema in mice when administered orally at doses of 3 and 10 mg/kg or intraperitoneally at doses of 0.3 and 1 mg/kg. SSR 240612 (10 mg/kg per day) reduces fibrosis in a unilateral ureteral obstruction mouse model of kidney fibrosis.{45046} It also reduces mean arterial blood pressure in two rat models of hypertension when administered at doses of 5 and 10 mg/kg and reduces plasma glucose and insulin levels in a glucose-fed rat model of insulin resistance when administered at a dose of 10 mg/kg per day.{45047,45048} SSR 240612 also exhibits analgesic properties in several rodent models of hyperalgesia.{45045}
Brand:CaymanSKU:25544 - 10 mgAvailable on backorder
SSR 240612 is a selective, non-peptide antagonist of the bradykinin B1 receptor (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).{45045} It inhibits the contraction of rabbit aorta and rat ileum induced by the B1 receptor agonist des-Arg9-bradykinin (des-Arg9-BK) ex vivo in a concentration-dependent manner. SSR 240612 (0.3 mg/kg) reduces tissue damage and neutrophil accumulation in a rat model of splanchnic artery occlusion/reperfusion-induced intestinal injury and inhibits des-Arg9-BK-induced paw edema in mice when administered orally at doses of 3 and 10 mg/kg or intraperitoneally at doses of 0.3 and 1 mg/kg. SSR 240612 (10 mg/kg per day) reduces fibrosis in a unilateral ureteral obstruction mouse model of kidney fibrosis.{45046} It also reduces mean arterial blood pressure in two rat models of hypertension when administered at doses of 5 and 10 mg/kg and reduces plasma glucose and insulin levels in a glucose-fed rat model of insulin resistance when administered at a dose of 10 mg/kg per day.{45047,45048} SSR 240612 also exhibits analgesic properties in several rodent models of hyperalgesia.{45045}
Brand:CaymanSKU:25544 - 25 mgAvailable on backorder
SSR 240612 is a selective, non-peptide antagonist of the bradykinin B1 receptor (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).{45045} It inhibits the contraction of rabbit aorta and rat ileum induced by the B1 receptor agonist des-Arg9-bradykinin (des-Arg9-BK) ex vivo in a concentration-dependent manner. SSR 240612 (0.3 mg/kg) reduces tissue damage and neutrophil accumulation in a rat model of splanchnic artery occlusion/reperfusion-induced intestinal injury and inhibits des-Arg9-BK-induced paw edema in mice when administered orally at doses of 3 and 10 mg/kg or intraperitoneally at doses of 0.3 and 1 mg/kg. SSR 240612 (10 mg/kg per day) reduces fibrosis in a unilateral ureteral obstruction mouse model of kidney fibrosis.{45046} It also reduces mean arterial blood pressure in two rat models of hypertension when administered at doses of 5 and 10 mg/kg and reduces plasma glucose and insulin levels in a glucose-fed rat model of insulin resistance when administered at a dose of 10 mg/kg per day.{45047,45048} SSR 240612 also exhibits analgesic properties in several rodent models of hyperalgesia.{45045}
Brand:CaymanSKU:25544 - 5 mgAvailable on backorder
SSR 69071 is a potent inhibitor of neutrophil elastase (Ki = 0.0168 nM for the human enzyme).{35315} It is selective for human neutrophil elastase over rat, mouse, and rabbit elastases (Kis = 3, 1.8, 58 nM, respectively). It inhibits human neutrophil elastase ex vivo in mouse bronchoalveolar lavage (BAL) fluid (ED50 = 10.5 mg/kg, p.o.). In vivo, SSR 69071 (2.8 mg/kg, p.o.) reduces acute lung hemorrhage induced by human neutrophil elastase in mice. It reduces carrageenan- and human neutrophil elastase-induced paw edema in rats (ED30s = 2.2 and 2.7 mg/kg, respectively). SSR 69071 also reduces cardiac infarct size when administered prior to ischemia or reperfusion in a rabbit model of ischemia-reperfusion injury.{35314}
Brand:CaymanSKU:21477 -Out of stock
SSR 69071 is a potent inhibitor of neutrophil elastase (Ki = 0.0168 nM for the human enzyme).{35315} It is selective for human neutrophil elastase over rat, mouse, and rabbit elastases (Kis = 3, 1.8, 58 nM, respectively). It inhibits human neutrophil elastase ex vivo in mouse bronchoalveolar lavage (BAL) fluid (ED50 = 10.5 mg/kg, p.o.). In vivo, SSR 69071 (2.8 mg/kg, p.o.) reduces acute lung hemorrhage induced by human neutrophil elastase in mice. It reduces carrageenan- and human neutrophil elastase-induced paw edema in rats (ED30s = 2.2 and 2.7 mg/kg, respectively). SSR 69071 also reduces cardiac infarct size when administered prior to ischemia or reperfusion in a rabbit model of ischemia-reperfusion injury.{35314}
Brand:CaymanSKU:21477 -Out of stock
SSR 69071 is a potent inhibitor of neutrophil elastase (Ki = 0.0168 nM for the human enzyme).{35315} It is selective for human neutrophil elastase over rat, mouse, and rabbit elastases (Kis = 3, 1.8, 58 nM, respectively). It inhibits human neutrophil elastase ex vivo in mouse bronchoalveolar lavage (BAL) fluid (ED50 = 10.5 mg/kg, p.o.). In vivo, SSR 69071 (2.8 mg/kg, p.o.) reduces acute lung hemorrhage induced by human neutrophil elastase in mice. It reduces carrageenan- and human neutrophil elastase-induced paw edema in rats (ED30s = 2.2 and 2.7 mg/kg, respectively). SSR 69071 also reduces cardiac infarct size when administered prior to ischemia or reperfusion in a rabbit model of ischemia-reperfusion injury.{35314}
Brand:CaymanSKU:21477 -Out of stock