Cayman
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Apart from direct peroxisome proliferator-activated receptor γ (PPARγ) agonism, several PPARγ ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) at serine 273.{25001} This effect requires binding to the PPARγ ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor.{25002} It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.{25002}
Brand:CaymanSKU:11086 - 10 mgAvailable on backorder
Apart from direct peroxisome proliferator-activated receptor γ (PPARγ) agonism, several PPARγ ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) at serine 273.{25001} This effect requires binding to the PPARγ ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor.{25002} It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.{25002}
Brand:CaymanSKU:11086 - 25 mgAvailable on backorder
Apart from direct peroxisome proliferator-activated receptor γ (PPARγ) agonism, several PPARγ ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) at serine 273.{25001} This effect requires binding to the PPARγ ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor.{25002} It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.{25002}
Brand:CaymanSKU:11086 - 5 mgAvailable on backorder
SR 16832 is a dual-site covalent antagonist of peroxisome proliferator-activated receptor γ (PPARγ).{42885} It inhibits MRL20-induced allosteric activation of PPARγ in a reporter assay using HEK293T cells when used at a concentration of 5 μM. SR 16832 also reduces basal activity of PPARγ and inhibits binding of docosahexaenoic acid (DHA; Item No. 90310) to PPARγ in a time-resolved FRET (TR-FRET) assay.
Brand:CaymanSKU:27632 - 1 mgAvailable on backorder
SR 16832 is a dual-site covalent antagonist of peroxisome proliferator-activated receptor γ (PPARγ).{42885} It inhibits MRL20-induced allosteric activation of PPARγ in a reporter assay using HEK293T cells when used at a concentration of 5 μM. SR 16832 also reduces basal activity of PPARγ and inhibits binding of docosahexaenoic acid (DHA; Item No. 90310) to PPARγ in a time-resolved FRET (TR-FRET) assay.
Brand:CaymanSKU:27632 - 10 mgAvailable on backorder
SR 16832 is a dual-site covalent antagonist of peroxisome proliferator-activated receptor γ (PPARγ).{42885} It inhibits MRL20-induced allosteric activation of PPARγ in a reporter assay using HEK293T cells when used at a concentration of 5 μM. SR 16832 also reduces basal activity of PPARγ and inhibits binding of docosahexaenoic acid (DHA; Item No. 90310) to PPARγ in a time-resolved FRET (TR-FRET) assay.
Brand:CaymanSKU:27632 - 25 mgAvailable on backorder
SR 16832 is a dual-site covalent antagonist of peroxisome proliferator-activated receptor γ (PPARγ).{42885} It inhibits MRL20-induced allosteric activation of PPARγ in a reporter assay using HEK293T cells when used at a concentration of 5 μM. SR 16832 also reduces basal activity of PPARγ and inhibits binding of docosahexaenoic acid (DHA; Item No. 90310) to PPARγ in a time-resolved FRET (TR-FRET) assay.
Brand:CaymanSKU:27632 - 5 mgAvailable on backorder
SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.
Brand:CaymanSKU:24480 - 1 mgAvailable on backorder
SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.
Brand:CaymanSKU:24480 - 10 mgAvailable on backorder
SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.
Brand:CaymanSKU:24480 - 25 mgAvailable on backorder
SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.
Brand:CaymanSKU:24480 - 5 mgAvailable on backorder
Peroxisome proliferator-activated receptor γ (PPARγ) is activated by the anti-diabetes drugs known as thiazolidinediones, including rosiglitazone (Item No. 71740) and pioglitazone (Item No. 71745).{8461} Phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) causes dysregulation of genes whose expression is altered in obesity, including adiponectin.{18956} SR 1824 is a non-agonist PPARγ ligand (Ki = 10 nM) which blocks Cdk5-mediated phosphorylation.{20015} It does not inhibit activation of PPARγ by rosiglitazone (Item No. 71740).{20015}
Brand:CaymanSKU:11087 - 1 mgAvailable on backorder
Peroxisome proliferator-activated receptor γ (PPARγ) is activated by the anti-diabetes drugs known as thiazolidinediones, including rosiglitazone (Item No. 71740) and pioglitazone (Item No. 71745).{8461} Phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) causes dysregulation of genes whose expression is altered in obesity, including adiponectin.{18956} SR 1824 is a non-agonist PPARγ ligand (Ki = 10 nM) which blocks Cdk5-mediated phosphorylation.{20015} It does not inhibit activation of PPARγ by rosiglitazone (Item No. 71740).{20015}
Brand:CaymanSKU:11087 - 10 mgAvailable on backorder
Peroxisome proliferator-activated receptor γ (PPARγ) is activated by the anti-diabetes drugs known as thiazolidinediones, including rosiglitazone (Item No. 71740) and pioglitazone (Item No. 71745).{8461} Phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) causes dysregulation of genes whose expression is altered in obesity, including adiponectin.{18956} SR 1824 is a non-agonist PPARγ ligand (Ki = 10 nM) which blocks Cdk5-mediated phosphorylation.{20015} It does not inhibit activation of PPARγ by rosiglitazone (Item No. 71740).{20015}
Brand:CaymanSKU:11087 - 25 mgAvailable on backorder
Peroxisome proliferator-activated receptor γ (PPARγ) is activated by the anti-diabetes drugs known as thiazolidinediones, including rosiglitazone (Item No. 71740) and pioglitazone (Item No. 71745).{8461} Phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) causes dysregulation of genes whose expression is altered in obesity, including adiponectin.{18956} SR 1824 is a non-agonist PPARγ ligand (Ki = 10 nM) which blocks Cdk5-mediated phosphorylation.{20015} It does not inhibit activation of PPARγ by rosiglitazone (Item No. 71740).{20015}
Brand:CaymanSKU:11087 - 5 mgAvailable on backorder
SR 18292 is an inhibitor of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α), a coactivator of transcription factors for genes involved in gluconeogenesis.{37125} SR 18292 (20 µM) increases acetylation of PGC-1α and, subsequently, decreases mRNA expression of phosphoenolpyruvate carboxykinase 1 (PEPCK1/Pck1) and the glucose-6-phosphatase catalytic subunit (G6Pc) in primary hepatocytes following stimulation with glucagon. In a dietary model of type II diabetes mellitus in mice, SR 18292 (45 mg/kg, i.p., for four days) reduces fasting blood glucose levels and the expression of liver Pck1. It also enhances glucose tolerance and insulin sensitivity in two mouse models of obesity.
Brand:CaymanSKU:22084 -Out of stock
SR 18292 is an inhibitor of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α), a coactivator of transcription factors for genes involved in gluconeogenesis.{37125} SR 18292 (20 µM) increases acetylation of PGC-1α and, subsequently, decreases mRNA expression of phosphoenolpyruvate carboxykinase 1 (PEPCK1/Pck1) and the glucose-6-phosphatase catalytic subunit (G6Pc) in primary hepatocytes following stimulation with glucagon. In a dietary model of type II diabetes mellitus in mice, SR 18292 (45 mg/kg, i.p., for four days) reduces fasting blood glucose levels and the expression of liver Pck1. It also enhances glucose tolerance and insulin sensitivity in two mouse models of obesity.
Brand:CaymanSKU:22084 -Out of stock
SR 18292 is an inhibitor of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α), a coactivator of transcription factors for genes involved in gluconeogenesis.{37125} SR 18292 (20 µM) increases acetylation of PGC-1α and, subsequently, decreases mRNA expression of phosphoenolpyruvate carboxykinase 1 (PEPCK1/Pck1) and the glucose-6-phosphatase catalytic subunit (G6Pc) in primary hepatocytes following stimulation with glucagon. In a dietary model of type II diabetes mellitus in mice, SR 18292 (45 mg/kg, i.p., for four days) reduces fasting blood glucose levels and the expression of liver Pck1. It also enhances glucose tolerance and insulin sensitivity in two mouse models of obesity.
Brand:CaymanSKU:22084 -Out of stock
SR 18292 is an inhibitor of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α), a coactivator of transcription factors for genes involved in gluconeogenesis.{37125} SR 18292 (20 µM) increases acetylation of PGC-1α and, subsequently, decreases mRNA expression of phosphoenolpyruvate carboxykinase 1 (PEPCK1/Pck1) and the glucose-6-phosphatase catalytic subunit (G6Pc) in primary hepatocytes following stimulation with glucagon. In a dietary model of type II diabetes mellitus in mice, SR 18292 (45 mg/kg, i.p., for four days) reduces fasting blood glucose levels and the expression of liver Pck1. It also enhances glucose tolerance and insulin sensitivity in two mouse models of obesity.
Brand:CaymanSKU:22084 -Out of stock
SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).{35980} It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.
Brand:CaymanSKU:28253 - 1 mgAvailable on backorder
SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).{35980} It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.
Brand:CaymanSKU:28253 - 10 mgAvailable on backorder
SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).{35980} It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.
Brand:CaymanSKU:28253 - 5 mgAvailable on backorder
SR 202 is an antagonist of peroxisome proliferator-activated receptor γ (PPARγ) transcriptional activity induced by troglitazone (Item No. 71750; IC50 = 140 µM) but not of basal PPARγ activity.{10768} It is selective for PPARγ, not affecting basal or agonist-induced transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). It inhibits PPARγ-dependent differentiation of preadipocyte 3T3-L1 cells in a dose-dependent manner. SR 202 (400 mg/kg) decreases the amount of weight gained and white adipose tissue mass accumulated by mice fed a standard or high-fat diet for ten weeks and is associated with lower PPARγ mRNA levels. It protects against high-fat diet-induced insulin resistance in wild-type mice and improves insulin sensitivity in ob/ob mice.
Brand:CaymanSKU:21846 -Out of stock
SR 202 is an antagonist of peroxisome proliferator-activated receptor γ (PPARγ) transcriptional activity induced by troglitazone (Item No. 71750; IC50 = 140 µM) but not of basal PPARγ activity.{10768} It is selective for PPARγ, not affecting basal or agonist-induced transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). It inhibits PPARγ-dependent differentiation of preadipocyte 3T3-L1 cells in a dose-dependent manner. SR 202 (400 mg/kg) decreases the amount of weight gained and white adipose tissue mass accumulated by mice fed a standard or high-fat diet for ten weeks and is associated with lower PPARγ mRNA levels. It protects against high-fat diet-induced insulin resistance in wild-type mice and improves insulin sensitivity in ob/ob mice.
Brand:CaymanSKU:21846 -Out of stock
Retinoic acid receptor-related nuclear receptor γ (RORγ) plays a central role in T cell differentiation, particularly in the differentiation of pro-inflammatory TH17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis.{19869,19493} SR 2211 selectively binds RORγ (Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORγ activity (IC50 = 320 nM).{21866} It has minimal effects on RORα, LXRα, and FXR activities. SR 2211 significantly inhibits gene expression of IL-17 and IL-23 receptor in activated EL-4 mouse T lymphocytes when given at 5 μM.{21866}
Brand:CaymanSKU:11972 - 1 mgAvailable on backorder
Retinoic acid receptor-related nuclear receptor γ (RORγ) plays a central role in T cell differentiation, particularly in the differentiation of pro-inflammatory TH17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis.{19869,19493} SR 2211 selectively binds RORγ (Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORγ activity (IC50 = 320 nM).{21866} It has minimal effects on RORα, LXRα, and FXR activities. SR 2211 significantly inhibits gene expression of IL-17 and IL-23 receptor in activated EL-4 mouse T lymphocytes when given at 5 μM.{21866}
Brand:CaymanSKU:11972 - 10 mgAvailable on backorder
Retinoic acid receptor-related nuclear receptor γ (RORγ) plays a central role in T cell differentiation, particularly in the differentiation of pro-inflammatory TH17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis.{19869,19493} SR 2211 selectively binds RORγ (Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORγ activity (IC50 = 320 nM).{21866} It has minimal effects on RORα, LXRα, and FXR activities. SR 2211 significantly inhibits gene expression of IL-17 and IL-23 receptor in activated EL-4 mouse T lymphocytes when given at 5 μM.{21866}
Brand:CaymanSKU:11972 - 5 mgAvailable on backorder
SR 2595 is an inverse agonist of PPARγ (IC50 = 30 nM) that represses both transactivation in a promoter:reporter assay and expression of the adipogenic marker fatty acid-binding protein 4 in differentiating murine preadipocytes.{29288} Repression of PPARγ with SR 2595 promotes osteogenesis, as measured by calcium phosphatase deposition, in cultured human mesenchymal stem cells (MSCs).{29288} SR 2595 also increases expression of bone morphogenetic proteins BMP2 and BMP6 in MSCs.{29288}
Brand:CaymanSKU:-Available on backorder
SR 2595 is an inverse agonist of PPARγ (IC50 = 30 nM) that represses both transactivation in a promoter:reporter assay and expression of the adipogenic marker fatty acid-binding protein 4 in differentiating murine preadipocytes.{29288} Repression of PPARγ with SR 2595 promotes osteogenesis, as measured by calcium phosphatase deposition, in cultured human mesenchymal stem cells (MSCs).{29288} SR 2595 also increases expression of bone morphogenetic proteins BMP2 and BMP6 in MSCs.{29288}
Brand:CaymanSKU:-Available on backorder
SR 2595 is an inverse agonist of PPARγ (IC50 = 30 nM) that represses both transactivation in a promoter:reporter assay and expression of the adipogenic marker fatty acid-binding protein 4 in differentiating murine preadipocytes.{29288} Repression of PPARγ with SR 2595 promotes osteogenesis, as measured by calcium phosphatase deposition, in cultured human mesenchymal stem cells (MSCs).{29288} SR 2595 also increases expression of bone morphogenetic proteins BMP2 and BMP6 in MSCs.{29288}
Brand:CaymanSKU:-Available on backorder
SR 27897 is a nonpeptide cholecystokinin (CCK) receptor antagonist.{42981} It selectively binds to CCK1 receptors in rat pancreatic membranes (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortical membranes and gastrin receptors in guinea pig gastric gland suspensions (IC50s = 489 and 2,883 nM, respectively). SR 27897 inhibits amylase secretion induced by CCK in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced guinea pig gallbladder contractions ex vivo (pA2 = 9.57). It completely reverses CCK-induced amylase secretion in rats when administered at a dose of 1 mg/kg. SR 27897 also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). SR 27897 inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 μg/kg).
Brand:CaymanSKU:28511 - 10 mgAvailable on backorder
SR 27897 is a nonpeptide cholecystokinin (CCK) receptor antagonist.{42981} It selectively binds to CCK1 receptors in rat pancreatic membranes (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortical membranes and gastrin receptors in guinea pig gastric gland suspensions (IC50s = 489 and 2,883 nM, respectively). SR 27897 inhibits amylase secretion induced by CCK in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced guinea pig gallbladder contractions ex vivo (pA2 = 9.57). It completely reverses CCK-induced amylase secretion in rats when administered at a dose of 1 mg/kg. SR 27897 also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). SR 27897 inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 μg/kg).
Brand:CaymanSKU:28511 - 25 mgAvailable on backorder
SR 27897 is a nonpeptide cholecystokinin (CCK) receptor antagonist.{42981} It selectively binds to CCK1 receptors in rat pancreatic membranes (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortical membranes and gastrin receptors in guinea pig gastric gland suspensions (IC50s = 489 and 2,883 nM, respectively). SR 27897 inhibits amylase secretion induced by CCK in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced guinea pig gallbladder contractions ex vivo (pA2 = 9.57). It completely reverses CCK-induced amylase secretion in rats when administered at a dose of 1 mg/kg. SR 27897 also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). SR 27897 inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 μg/kg).
Brand:CaymanSKU:28511 - 5 mgAvailable on backorder
SR 27897 is a nonpeptide cholecystokinin (CCK) receptor antagonist.{42981} It selectively binds to CCK1 receptors in rat pancreatic membranes (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortical membranes and gastrin receptors in guinea pig gastric gland suspensions (IC50s = 489 and 2,883 nM, respectively). SR 27897 inhibits amylase secretion induced by CCK in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced guinea pig gallbladder contractions ex vivo (pA2 = 9.57). It completely reverses CCK-induced amylase secretion in rats when administered at a dose of 1 mg/kg. SR 27897 also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). SR 27897 inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 μg/kg).
Brand:CaymanSKU:28511 - 50 mgAvailable on backorder
SR 3029 is an inhibitor of casein kinase 1δ (CK1δ) and CK1ε (IC50s = 44 and 260 nM, respectively).{47522} It is selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by greater than 90% at 10 µM. SR 3029 inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 with IC50 values of 576, 368, 428, 427, and 3,000 nM, respectively. It inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM). SR 3029 (20 mg/kg per day) reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models.{47523} It reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue.
Brand:CaymanSKU:27048 - 10 mgAvailable on backorder
SR 3029 is an inhibitor of casein kinase 1δ (CK1δ) and CK1ε (IC50s = 44 and 260 nM, respectively).{47522} It is selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by greater than 90% at 10 µM. SR 3029 inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 with IC50 values of 576, 368, 428, 427, and 3,000 nM, respectively. It inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM). SR 3029 (20 mg/kg per day) reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models.{47523} It reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue.
Brand:CaymanSKU:27048 - 25 mgAvailable on backorder
SR 3029 is an inhibitor of casein kinase 1δ (CK1δ) and CK1ε (IC50s = 44 and 260 nM, respectively).{47522} It is selective for CK1δ and CK1ε over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by greater than 90% at 10 µM. SR 3029 inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 with IC50 values of 576, 368, 428, 427, and 3,000 nM, respectively. It inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM). SR 3029 (20 mg/kg per day) reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models.{47523} It reduces the expression of the Wnt/β-catenin target CCND1 and decreases protein levels of nuclear β-catenin and cyclin D1 in mouse tumor tissue.
Brand:CaymanSKU:27048 - 5 mgAvailable on backorder
The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles.{19493,19955,19869} SR 3335 is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM).{21470} It is without effect on RORβ, RORγ, farnesoid X receptor, or liver X receptor α. SR 3335 evokes RORα-dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis.{21470}
Brand:CaymanSKU:12072 - 1 mgAvailable on backorder
The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles.{19493,19955,19869} SR 3335 is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM).{21470} It is without effect on RORβ, RORγ, farnesoid X receptor, or liver X receptor α. SR 3335 evokes RORα-dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis.{21470}
Brand:CaymanSKU:12072 - 10 mgAvailable on backorder
The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles.{19493,19955,19869} SR 3335 is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM).{21470} It is without effect on RORβ, RORγ, farnesoid X receptor, or liver X receptor α. SR 3335 evokes RORα-dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis.{21470}
Brand:CaymanSKU:12072 - 25 mgAvailable on backorder
The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles.{19493,19955,19869} SR 3335 is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM).{21470} It is without effect on RORβ, RORγ, farnesoid X receptor, or liver X receptor α. SR 3335 evokes RORα-dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis.{21470}
Brand:CaymanSKU:12072 - 5 mgAvailable on backorder
SR 3576 is a JNK3 inhibitor (IC50 = 7 nM).{57073} It is selective for JNK3 over JNK1 and p38 MAP kinase (IC50s = 0.17 and >20 µM, respectively). It inhibits c-Jun phosphorylation in INS-1 cells (IC50 = 1.3 µM).
Brand:CaymanSKU:20215 -Available on backorder
SR 3576 is a JNK3 inhibitor (IC50 = 7 nM).{57073} It is selective for JNK3 over JNK1 and p38 MAP kinase (IC50s = 0.17 and >20 µM, respectively). It inhibits c-Jun phosphorylation in INS-1 cells (IC50 = 1.3 µM).
Brand:CaymanSKU:20215 -Available on backorder
SR 3677 is a potent, ATP-competitive inhibitor of Rho-associated kinases (ROCKs) that shows greater potency against ROCK-II than ROCK-I in enzyme and cell-based assays (IC50 values are 3 and 56 nM, respectively).{27385} At 3 µM, SR 3677 inhibits only 5 (Akt3, Clk1, Clk2, Clk4, Lats2) out of 353 kinases with greater than 50% inhibition.{27385} SR 3677 is efficacious at inhibiting myosin light chain phosphorylation and increasing aqueous humor outflow in porcine eyes in an ex vivo model of glaucoma treatment.{27385}
Brand:CaymanSKU:-Out of stock
SR 3677 is a potent, ATP-competitive inhibitor of Rho-associated kinases (ROCKs) that shows greater potency against ROCK-II than ROCK-I in enzyme and cell-based assays (IC50 values are 3 and 56 nM, respectively).{27385} At 3 µM, SR 3677 inhibits only 5 (Akt3, Clk1, Clk2, Clk4, Lats2) out of 353 kinases with greater than 50% inhibition.{27385} SR 3677 is efficacious at inhibiting myosin light chain phosphorylation and increasing aqueous humor outflow in porcine eyes in an ex vivo model of glaucoma treatment.{27385}
Brand:CaymanSKU:-Out of stock
SR 3677 is a potent, ATP-competitive inhibitor of Rho-associated kinases (ROCKs) that shows greater potency against ROCK-II than ROCK-I in enzyme and cell-based assays (IC50 values are 3 and 56 nM, respectively).{27385} At 3 µM, SR 3677 inhibits only 5 (Akt3, Clk1, Clk2, Clk4, Lats2) out of 353 kinases with greater than 50% inhibition.{27385} SR 3677 is efficacious at inhibiting myosin light chain phosphorylation and increasing aqueous humor outflow in porcine eyes in an ex vivo model of glaucoma treatment.{27385}
Brand:CaymanSKU:-Out of stock
SR 3677 is a potent, ATP-competitive inhibitor of Rho-associated kinases (ROCKs) that shows greater potency against ROCK-II than ROCK-I in enzyme and cell-based assays (IC50 values are 3 and 56 nM, respectively).{27385} At 3 µM, SR 3677 inhibits only 5 (Akt3, Clk1, Clk2, Clk4, Lats2) out of 353 kinases with greater than 50% inhibition.{27385} SR 3677 is efficacious at inhibiting myosin light chain phosphorylation and increasing aqueous humor outflow in porcine eyes in an ex vivo model of glaucoma treatment.{27385}
Brand:CaymanSKU:-Out of stock
SR 4370 is an inhibitor of histone deacetylase 3 (HDAC3; IC50 = 6 nM).{47684} It is selective for HDAC3 over HDAC1, -2, -6, and -8 (IC50s = 0.13, 0.58, 3.7, and 2.3 µM, respectively). SR 4370 decreases viability of MDA-MB-231 human breast cancer cells with an IC50 value of 12.6 µM.
Brand:CaymanSKU:25543 - 1 mgAvailable on backorder
SR 4370 is an inhibitor of histone deacetylase 3 (HDAC3; IC50 = 6 nM).{47684} It is selective for HDAC3 over HDAC1, -2, -6, and -8 (IC50s = 0.13, 0.58, 3.7, and 2.3 µM, respectively). SR 4370 decreases viability of MDA-MB-231 human breast cancer cells with an IC50 value of 12.6 µM.
Brand:CaymanSKU:25543 - 10 mgAvailable on backorder
SR 4370 is an inhibitor of histone deacetylase 3 (HDAC3; IC50 = 6 nM).{47684} It is selective for HDAC3 over HDAC1, -2, -6, and -8 (IC50s = 0.13, 0.58, 3.7, and 2.3 µM, respectively). SR 4370 decreases viability of MDA-MB-231 human breast cancer cells with an IC50 value of 12.6 µM.
Brand:CaymanSKU:25543 - 25 mgAvailable on backorder
SR 4370 is an inhibitor of histone deacetylase 3 (HDAC3; IC50 = 6 nM).{47684} It is selective for HDAC3 over HDAC1, -2, -6, and -8 (IC50s = 0.13, 0.58, 3.7, and 2.3 µM, respectively). SR 4370 decreases viability of MDA-MB-231 human breast cancer cells with an IC50 value of 12.6 µM.
Brand:CaymanSKU:25543 - 5 mgAvailable on backorder
SR 48692 is an orally bioavailable allosteric antagonist of the neurotensin receptor NTS1 (Kd = 3.4 nM).{35296,35297} SR 48692 inhibits high affinity neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as well as rat mesencephalic cells and HT-29 cells with IC50 values ranging from 0.99 to 30.3 nM.{35296} It blocks neurotensin-induced intracellular calcium mobilization in HT-29 cells with a Ki value of 7.4 nM. SR 48692 (10 μM) inhibits NCI-H209 and NCI-H345 cell proliferation by approximately 70 and 80%, respectively.{35299} In vivo, SR 48692 (10 μg per day) reduces tumor volume and cell proliferation in an NCI-H209 mouse xenograft model. SR 48692 (80 μg/kg, p.o.) reduces contralateral turning induced by neurotensin (Item No. 24717) administration in mice by 85%.{35296} Daily administration of SR 48692 for five days in rats delays sensitization to the locomotor activating effects of cocaine during three additional cocaine challenges when given seven days prior to cocaine delivery but not under a cotreatment regimen.{35298}
Brand:CaymanSKU:20124 -Available on backorder
SR 48692 is an orally bioavailable allosteric antagonist of the neurotensin receptor NTS1 (Kd = 3.4 nM).{35296,35297} SR 48692 inhibits high affinity neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as well as rat mesencephalic cells and HT-29 cells with IC50 values ranging from 0.99 to 30.3 nM.{35296} It blocks neurotensin-induced intracellular calcium mobilization in HT-29 cells with a Ki value of 7.4 nM. SR 48692 (10 μM) inhibits NCI-H209 and NCI-H345 cell proliferation by approximately 70 and 80%, respectively.{35299} In vivo, SR 48692 (10 μg per day) reduces tumor volume and cell proliferation in an NCI-H209 mouse xenograft model. SR 48692 (80 μg/kg, p.o.) reduces contralateral turning induced by neurotensin (Item No. 24717) administration in mice by 85%.{35296} Daily administration of SR 48692 for five days in rats delays sensitization to the locomotor activating effects of cocaine during three additional cocaine challenges when given seven days prior to cocaine delivery but not under a cotreatment regimen.{35298}
Brand:CaymanSKU:20124 -Available on backorder
SR 48692 is an orally bioavailable allosteric antagonist of the neurotensin receptor NTS1 (Kd = 3.4 nM).{35296,35297} SR 48692 inhibits high affinity neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as well as rat mesencephalic cells and HT-29 cells with IC50 values ranging from 0.99 to 30.3 nM.{35296} It blocks neurotensin-induced intracellular calcium mobilization in HT-29 cells with a Ki value of 7.4 nM. SR 48692 (10 μM) inhibits NCI-H209 and NCI-H345 cell proliferation by approximately 70 and 80%, respectively.{35299} In vivo, SR 48692 (10 μg per day) reduces tumor volume and cell proliferation in an NCI-H209 mouse xenograft model. SR 48692 (80 μg/kg, p.o.) reduces contralateral turning induced by neurotensin (Item No. 24717) administration in mice by 85%.{35296} Daily administration of SR 48692 for five days in rats delays sensitization to the locomotor activating effects of cocaine during three additional cocaine challenges when given seven days prior to cocaine delivery but not under a cotreatment regimen.{35298}
Brand:CaymanSKU:20124 -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 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