Chemicals
Showing 25501–25650 of 41137 results
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Losartan carboxaldehyde is an intermediate aldehyde metabolite of the angiotensin II type 1 receptor antagonist, losartan (Item No. 10006594). It does not block angiotensin receptors, but instead inhibits endothelial cyclooxygenase (COX)-2 expression, thereby exerting anti-inflammatory actions.{30560} At 1 µM in vitro, losartan carboxaldehyde has also been shown to block the upregulation of intercellular adhesion molecule (ICAM)-1 mRNA and COX-dependent generation of thromboxane A2 and prostaglandin F2α (Item No. 16010).{30560} Losartan carboxaldehyde can also act as a partial agonist (EC50 = 17.1 µM) of the insulin-sensitizing peroxisome proliferator-activated receptor γ in vitro.{30561,30559}
Brand:CaymanSKU:-Available on backorder
Losartan carboxaldehyde is an intermediate aldehyde metabolite of the angiotensin II type 1 receptor antagonist, losartan (Item No. 10006594). It does not block angiotensin receptors, but instead inhibits endothelial cyclooxygenase (COX)-2 expression, thereby exerting anti-inflammatory actions.{30560} At 1 µM in vitro, losartan carboxaldehyde has also been shown to block the upregulation of intercellular adhesion molecule (ICAM)-1 mRNA and COX-dependent generation of thromboxane A2 and prostaglandin F2α (Item No. 16010).{30560} Losartan carboxaldehyde can also act as a partial agonist (EC50 = 17.1 µM) of the insulin-sensitizing peroxisome proliferator-activated receptor γ in vitro.{30561,30559}
Brand:CaymanSKU:-Available on backorder
Losartan carboxaldehyde is an intermediate aldehyde metabolite of the angiotensin II type 1 receptor antagonist, losartan (Item No. 10006594). It does not block angiotensin receptors, but instead inhibits endothelial cyclooxygenase (COX)-2 expression, thereby exerting anti-inflammatory actions.{30560} At 1 µM in vitro, losartan carboxaldehyde has also been shown to block the upregulation of intercellular adhesion molecule (ICAM)-1 mRNA and COX-dependent generation of thromboxane A2 and prostaglandin F2α (Item No. 16010).{30560} Losartan carboxaldehyde can also act as a partial agonist (EC50 = 17.1 µM) of the insulin-sensitizing peroxisome proliferator-activated receptor γ in vitro.{30561,30559}
Brand:CaymanSKU:-Available on backorder
Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.{28030} Like the parent compound, losartan carboxylic acid is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.{28032,28031,21001} When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan.{21001} However, the metabolite has very low oral bioavailability.{21001} Losartan, but not its metabolite, inhibits platelet aggregation in vitro.{20999}
Brand:CaymanSKU:- Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.{28030} Like the parent compound, losartan carboxylic acid is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.{28032,28031,21001} When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan.{21001} However, the metabolite has very low oral bioavailability.{21001} Losartan, but not its metabolite, inhibits platelet aggregation in vitro.{20999}
Brand:CaymanSKU:- Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.{28030} Like the parent compound, losartan carboxylic acid is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.{28032,28031,21001} When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan.{21001} However, the metabolite has very low oral bioavailability.{21001} Losartan, but not its metabolite, inhibits platelet aggregation in vitro.{20999}
Brand:CaymanSKU:- Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.{28030} Like the parent compound, losartan carboxylic acid is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.{28032,28031,21001} When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan.{21001} However, the metabolite has very low oral bioavailability.{21001} Losartan, but not its metabolite, inhibits platelet aggregation in vitro.{20999}
Brand:CaymanSKU:-
Losartan-d4 contains four deuterium atoms located on the phenyl group. It is intended for use as an internal standard for the quantification of losartan (potassium salt) (Item No. 10006594) by GC- or LC-MS. Losartan is an antagonist of the angiotensin (AT) II receptor subtype AT1 with a Ki value of 5-20 nM.{12997} It has an attenuating effect on vein graft atherosclerosis in rabbits and effectively reduces arterial blood pressure in rats.{12998,13089} Formulations containing losartan have been used to control hypertension while protecting renal function.{12996}
Brand:CaymanSKU:22567 -Out of stock
Losartan-d4 contains four deuterium atoms located on the phenyl group. It is intended for use as an internal standard for the quantification of losartan (potassium salt) (Item No. 10006594) by GC- or LC-MS. Losartan is an antagonist of the angiotensin (AT) II receptor subtype AT1 with a Ki value of 5-20 nM.{12997} It has an attenuating effect on vein graft atherosclerosis in rabbits and effectively reduces arterial blood pressure in rats.{12998,13089} Formulations containing losartan have been used to control hypertension while protecting renal function.{12996}
Brand:CaymanSKU:22567 -Out of stock
Loteprednol etabonate is a glucocorticoid receptor agonist with an affinity 4.3 times that of dexamethasone (Item No. 11015).{40360} It decreases wound healing time in mice and minimizes scarring of rabbit cornea wounds.{40362,40361} Formulations containing loteprednol etabonate are used in the treatment of inflammatory eye conditions.
Brand:CaymanSKU:23305 - 10 mgAvailable on backorder
Loteprednol etabonate is a glucocorticoid receptor agonist with an affinity 4.3 times that of dexamethasone (Item No. 11015).{40360} It decreases wound healing time in mice and minimizes scarring of rabbit cornea wounds.{40362,40361} Formulations containing loteprednol etabonate are used in the treatment of inflammatory eye conditions.
Brand:CaymanSKU:23305 - 25 mgAvailable on backorder
Loteprednol etabonate is a glucocorticoid receptor agonist with an affinity 4.3 times that of dexamethasone (Item No. 11015).{40360} It decreases wound healing time in mice and minimizes scarring of rabbit cornea wounds.{40362,40361} Formulations containing loteprednol etabonate are used in the treatment of inflammatory eye conditions.
Brand:CaymanSKU:23305 - 5 mgAvailable on backorder
Loteprednol etabonate is a glucocorticoid receptor agonist with an affinity 4.3 times that of dexamethasone (Item No. 11015).{40360} It decreases wound healing time in mice and minimizes scarring of rabbit cornea wounds.{40362,40361} Formulations containing loteprednol etabonate are used in the treatment of inflammatory eye conditions.
Brand:CaymanSKU:23305 - 50 mgAvailable on backorder
Loureirin B is a flavonoid originally isolated from D. cochinchinensis, a major component of the traditional herbal medicine dragon’s blood, and has diverse biological activities.{48437,48438,48439} It inhibits Kv1.3-mediated currents, induces membrane depolarization, and reduces calcium influx in Jurkat T cells.{48437} It also inhibits phytohemagglutinin-induced IL-2 release from these cells. Loureirin B (25 μg/ml) reduces type I collagen and fibronectin protein levels in TGF-β1-stimulated fibroblasts as well as contraction of TGF-β1-stimulated fibroblasts in a gel contraction assay.{48438} It reduces type I collagen and fibronectin protein levels and inhibits phosphorylation of ERK and JNK in isolated human hypertrophic scar tissue. Loureirin B increases glucose absorption and intracellular ATP levels in Ins-1 cells via inhibition of the KATP current and intracellular influx of calcium.{48439}
Brand:CaymanSKU:27454 - 10 mgAvailable on backorder
Loureirin B is a flavonoid originally isolated from D. cochinchinensis, a major component of the traditional herbal medicine dragon’s blood, and has diverse biological activities.{48437,48438,48439} It inhibits Kv1.3-mediated currents, induces membrane depolarization, and reduces calcium influx in Jurkat T cells.{48437} It also inhibits phytohemagglutinin-induced IL-2 release from these cells. Loureirin B (25 μg/ml) reduces type I collagen and fibronectin protein levels in TGF-β1-stimulated fibroblasts as well as contraction of TGF-β1-stimulated fibroblasts in a gel contraction assay.{48438} It reduces type I collagen and fibronectin protein levels and inhibits phosphorylation of ERK and JNK in isolated human hypertrophic scar tissue. Loureirin B increases glucose absorption and intracellular ATP levels in Ins-1 cells via inhibition of the KATP current and intracellular influx of calcium.{48439}
Brand:CaymanSKU:27454 - 25 mgAvailable on backorder
Loureirin B is a flavonoid originally isolated from D. cochinchinensis, a major component of the traditional herbal medicine dragon’s blood, and has diverse biological activities.{48437,48438,48439} It inhibits Kv1.3-mediated currents, induces membrane depolarization, and reduces calcium influx in Jurkat T cells.{48437} It also inhibits phytohemagglutinin-induced IL-2 release from these cells. Loureirin B (25 μg/ml) reduces type I collagen and fibronectin protein levels in TGF-β1-stimulated fibroblasts as well as contraction of TGF-β1-stimulated fibroblasts in a gel contraction assay.{48438} It reduces type I collagen and fibronectin protein levels and inhibits phosphorylation of ERK and JNK in isolated human hypertrophic scar tissue. Loureirin B increases glucose absorption and intracellular ATP levels in Ins-1 cells via inhibition of the KATP current and intracellular influx of calcium.{48439}
Brand:CaymanSKU:27454 - 5 mgAvailable on backorder
Loureirin B is a flavonoid originally isolated from D. cochinchinensis, a major component of the traditional herbal medicine dragon’s blood, and has diverse biological activities.{48437,48438,48439} It inhibits Kv1.3-mediated currents, induces membrane depolarization, and reduces calcium influx in Jurkat T cells.{48437} It also inhibits phytohemagglutinin-induced IL-2 release from these cells. Loureirin B (25 μg/ml) reduces type I collagen and fibronectin protein levels in TGF-β1-stimulated fibroblasts as well as contraction of TGF-β1-stimulated fibroblasts in a gel contraction assay.{48438} It reduces type I collagen and fibronectin protein levels and inhibits phosphorylation of ERK and JNK in isolated human hypertrophic scar tissue. Loureirin B increases glucose absorption and intracellular ATP levels in Ins-1 cells via inhibition of the KATP current and intracellular influx of calcium.{48439}
Brand:CaymanSKU:27454 - 50 mgAvailable on backorder
Lovastatin is an HMG-CoA reductase inhibitor that was initially isolated from A. terreus.{15081} It is a prodrug of its more potent metabolite, lovastatin hydroxy acid (Item No. 10010339). Both competitively inhibit HMG-CoA reductase with Ki values of 1.4 and 0.6 nM for lovastatin and the open ring, hydroxy acid form, respectively.{15251} Lovastatin (8 mg/kg/day) reduces plasma cholesterol in dogs by 29% over a three week period. It also suppresses TNF-induced NF-κB activation (IC50 ~ 15 µM), which potentiates apoptosis in human myeloid leukemia cells and thus, may be useful in treating cancer.{15363} Formulations containing lovastatin were the first HMG-CoA reductase inhibitors to be used in the treatment of hypercholesterolemia.
Brand:CaymanSKU:10010338 - 10 mgAvailable on backorder
Lovastatin is an HMG-CoA reductase inhibitor that was initially isolated from A. terreus.{15081} It is a prodrug of its more potent metabolite, lovastatin hydroxy acid (Item No. 10010339). Both competitively inhibit HMG-CoA reductase with Ki values of 1.4 and 0.6 nM for lovastatin and the open ring, hydroxy acid form, respectively.{15251} Lovastatin (8 mg/kg/day) reduces plasma cholesterol in dogs by 29% over a three week period. It also suppresses TNF-induced NF-κB activation (IC50 ~ 15 µM), which potentiates apoptosis in human myeloid leukemia cells and thus, may be useful in treating cancer.{15363} Formulations containing lovastatin were the first HMG-CoA reductase inhibitors to be used in the treatment of hypercholesterolemia.
Brand:CaymanSKU:10010338 - 5 mgAvailable on backorder
Lovastatin is an HMG-CoA reductase inhibitor that was initially isolated from A. terreus.{15081} It is a prodrug of its more potent metabolite, lovastatin hydroxy acid (Item No. 10010339). Both competitively inhibit HMG-CoA reductase with Ki values of 1.4 and 0.6 nM for lovastatin and the open ring, hydroxy acid form, respectively.{15251} Lovastatin (8 mg/kg/day) reduces plasma cholesterol in dogs by 29% over a three week period. It also suppresses TNF-induced NF-κB activation (IC50 ~ 15 µM), which potentiates apoptosis in human myeloid leukemia cells and thus, may be useful in treating cancer.{15363} Formulations containing lovastatin were the first HMG-CoA reductase inhibitors to be used in the treatment of hypercholesterolemia.
Brand:CaymanSKU:10010338 - 50 mgAvailable on backorder
Lovastatin hydroxy acid is a potent and competitive inhibitor of HMG-CoA reductase (Ki = 0.6 nM).{15251} It is the more potent, open ring, hydroxy acid form of its prodrug, lovastatin (Item No. 10010338).{39152}
Brand:CaymanSKU:10010339 - 1 mgAvailable on backorder
Lovastatin hydroxy acid is a potent and competitive inhibitor of HMG-CoA reductase (Ki = 0.6 nM).{15251} It is the more potent, open ring, hydroxy acid form of its prodrug, lovastatin (Item No. 10010338).{39152}
Brand:CaymanSKU:10010339 - 10 mgAvailable on backorder
Lovastatin hydroxy acid is a potent and competitive inhibitor of HMG-CoA reductase (Ki = 0.6 nM).{15251} It is the more potent, open ring, hydroxy acid form of its prodrug, lovastatin (Item No. 10010338).{39152}
Brand:CaymanSKU:10010339 - 25 mgAvailable on backorder
Lovastatin hydroxy acid is a potent and competitive inhibitor of HMG-CoA reductase (Ki = 0.6 nM).{15251} It is the more potent, open ring, hydroxy acid form of its prodrug, lovastatin (Item No. 10010338).{39152}
Brand:CaymanSKU:10010339 - 5 mgAvailable on backorder
Loxapine is an atypical antipsychotic drug that displays high affinity for histamine, 5-HT, dopamine, and α1-adrenergic receptors (Ki values are 7, 7.7, 9.5, 12, and 31 nM for H1, 5-HT2A, 5-HT2C, D2, and α1A, respectively).{24252,24253} It reduces agitation associated with schizophrenia or bipolar disorder.{32724}
Brand:CaymanSKU:20760 -Available on backorder
Loxapine is an atypical antipsychotic drug that displays high affinity for histamine, 5-HT, dopamine, and α1-adrenergic receptors (Ki values are 7, 7.7, 9.5, 12, and 31 nM for H1, 5-HT2A, 5-HT2C, D2, and α1A, respectively).{24252,24253} It reduces agitation associated with schizophrenia or bipolar disorder.{32724}
Brand:CaymanSKU:20760 -Available on backorder
Loxapine is an atypical antipsychotic drug that displays high affinity for histamine, 5-HT, dopamine, and α1-adrenergic receptors (Ki values are 7, 7.7, 9.5, 12, and 31 nM for H1, 5-HT2A, 5-HT2C, D2, and α1A, respectively).{24252,24253} It reduces agitation associated with schizophrenia or bipolar disorder.{32724}
Brand:CaymanSKU:20760 -Available on backorder
Loxiglumide is a cholecystokinin (CCK) receptor antagonist that inhibits CCK-8 binding to central and peripheral CCK receptors with Ki values of 9.1 and 0.33 μM, respectively.{41979} It inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladder (IC50 = 10 nM).{41980} Loxiglumide (50 μM) reduces the invasion of PANC-1 and MiaPaCa-2 human pancreatic cancer cells by 83.1 and 82.9%, respectively, in vitro.{41981} Loxiglumide (10-5,000 μM) reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells in a concentration-dependent manner (IC50s = 160 and 74 μM, respectively).{41982} It reduces the tumor growth rate by 37.5 and 38%, respectively, in PC-TI and PC-YY mouse xenograft models when administered at a dose of 250 mg/kg. Loxiglumide is toxic to mice with LD50 values ranging from 440 to 500 mg/kg dependent on the route of administration. In a rat model of acute pancreatitis, loxiglumide (50 mg/kg, s.c.) reduces serum concentrations of CCK, amylase, and lipase by greater than 60%, as well as tissue hemorrhaging and acinar cell necrosis.{41983}
Brand:CaymanSKU:25534 - 10 mgAvailable on backorder
Loxiglumide is a cholecystokinin (CCK) receptor antagonist that inhibits CCK-8 binding to central and peripheral CCK receptors with Ki values of 9.1 and 0.33 μM, respectively.{41979} It inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladder (IC50 = 10 nM).{41980} Loxiglumide (50 μM) reduces the invasion of PANC-1 and MiaPaCa-2 human pancreatic cancer cells by 83.1 and 82.9%, respectively, in vitro.{41981} Loxiglumide (10-5,000 μM) reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells in a concentration-dependent manner (IC50s = 160 and 74 μM, respectively).{41982} It reduces the tumor growth rate by 37.5 and 38%, respectively, in PC-TI and PC-YY mouse xenograft models when administered at a dose of 250 mg/kg. Loxiglumide is toxic to mice with LD50 values ranging from 440 to 500 mg/kg dependent on the route of administration. In a rat model of acute pancreatitis, loxiglumide (50 mg/kg, s.c.) reduces serum concentrations of CCK, amylase, and lipase by greater than 60%, as well as tissue hemorrhaging and acinar cell necrosis.{41983}
Brand:CaymanSKU:25534 - 25 mgAvailable on backorder
Loxiglumide is a cholecystokinin (CCK) receptor antagonist that inhibits CCK-8 binding to central and peripheral CCK receptors with Ki values of 9.1 and 0.33 μM, respectively.{41979} It inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladder (IC50 = 10 nM).{41980} Loxiglumide (50 μM) reduces the invasion of PANC-1 and MiaPaCa-2 human pancreatic cancer cells by 83.1 and 82.9%, respectively, in vitro.{41981} Loxiglumide (10-5,000 μM) reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells in a concentration-dependent manner (IC50s = 160 and 74 μM, respectively).{41982} It reduces the tumor growth rate by 37.5 and 38%, respectively, in PC-TI and PC-YY mouse xenograft models when administered at a dose of 250 mg/kg. Loxiglumide is toxic to mice with LD50 values ranging from 440 to 500 mg/kg dependent on the route of administration. In a rat model of acute pancreatitis, loxiglumide (50 mg/kg, s.c.) reduces serum concentrations of CCK, amylase, and lipase by greater than 60%, as well as tissue hemorrhaging and acinar cell necrosis.{41983}
Brand:CaymanSKU:25534 - 5 mgAvailable on backorder
Loxiglumide is a cholecystokinin (CCK) receptor antagonist that inhibits CCK-8 binding to central and peripheral CCK receptors with Ki values of 9.1 and 0.33 μM, respectively.{41979} It inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladder (IC50 = 10 nM).{41980} Loxiglumide (50 μM) reduces the invasion of PANC-1 and MiaPaCa-2 human pancreatic cancer cells by 83.1 and 82.9%, respectively, in vitro.{41981} Loxiglumide (10-5,000 μM) reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells in a concentration-dependent manner (IC50s = 160 and 74 μM, respectively).{41982} It reduces the tumor growth rate by 37.5 and 38%, respectively, in PC-TI and PC-YY mouse xenograft models when administered at a dose of 250 mg/kg. Loxiglumide is toxic to mice with LD50 values ranging from 440 to 500 mg/kg dependent on the route of administration. In a rat model of acute pancreatitis, loxiglumide (50 mg/kg, s.c.) reduces serum concentrations of CCK, amylase, and lipase by greater than 60%, as well as tissue hemorrhaging and acinar cell necrosis.{41983}
Brand:CaymanSKU:25534 - 50 mgAvailable on backorder
LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM).{42680} It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
Brand:CaymanSKU:27056 - 1 mgAvailable on backorder
LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM).{42680} It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
Brand:CaymanSKU:27056 - 10 mgAvailable on backorder
LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM).{42680} It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
Brand:CaymanSKU:27056 - 25 mgAvailable on backorder
LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM).{42680} It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
Brand:CaymanSKU:27056 - 5 mgAvailable on backorder
LOXO-195 is an inhibitor of the receptor tyrosine kinases TrkA and TrkC (IC50s = 0.6 and G595R, TrkAG667C, TrkCG623R, and TrkCG696A (IC50s = 2, 9.8, 2.3, and 50 value of 1.9 nM. It selectively inhibits proliferation of Trk fusion-positive K12, CUTO-3, and MO-91 cell lines (IC50s = ≤5 nM) over Trk fusion-negative cell lines when used at concentrations up to 10 μM. LOXO-195 (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.
Brand:CaymanSKU:27062 - 1 mgAvailable on backorder
LOXO-195 is an inhibitor of the receptor tyrosine kinases TrkA and TrkC (IC50s = 0.6 and G595R, TrkAG667C, TrkCG623R, and TrkCG696A (IC50s = 2, 9.8, 2.3, and 50 value of 1.9 nM. It selectively inhibits proliferation of Trk fusion-positive K12, CUTO-3, and MO-91 cell lines (IC50s = ≤5 nM) over Trk fusion-negative cell lines when used at concentrations up to 10 μM. LOXO-195 (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.
Brand:CaymanSKU:27062 - 10 mgAvailable on backorder
LOXO-195 is an inhibitor of the receptor tyrosine kinases TrkA and TrkC (IC50s = 0.6 and G595R, TrkAG667C, TrkCG623R, and TrkCG696A (IC50s = 2, 9.8, 2.3, and 50 value of 1.9 nM. It selectively inhibits proliferation of Trk fusion-positive K12, CUTO-3, and MO-91 cell lines (IC50s = ≤5 nM) over Trk fusion-negative cell lines when used at concentrations up to 10 μM. LOXO-195 (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.
Brand:CaymanSKU:27062 - 5 mgAvailable on backorder
Loxoribine is a guanosine derivative and an agonist of toll-like receptor 7 (TLR7).{42514,42515} It is selective for TLR7 over other human TLRs in a cell-based reporter assay at 1 mM.{42515}. Loxoribine induces proliferation, increases the antibody response to sheep red blood cells, and activates natural killer cell activity against Yac-1 lymphoma cells in murine splenocyte cultures (EC50s = 10-50, 3-20, and 13-22 μM, respectively).{42514} Loxoribine (250 μM) increases production of IL-12, IL-23, IL-27, and IL-10 by human monocyte-derived dendritic cells (MoDCs).{42516} Loxoribine-treated MoDCs induce higher levels of IL-17 and IFN-γ secretion by co-cultured allogeneic CD4+ T cells compared to control MoDCs. Loxoribine (120 mg/kg) reduces the number of pulmonary metastases in the B16 mouse model of melanoma, an effect enhanced by co-administration of IL-2, and exhibits adjuvant activity in mice immunized with a B16 tumor vaccine.{42517}
Brand:CaymanSKU:21186 -Out of stock
Loxoribine is a guanosine derivative and an agonist of toll-like receptor 7 (TLR7).{42514,42515} It is selective for TLR7 over other human TLRs in a cell-based reporter assay at 1 mM.{42515}. Loxoribine induces proliferation, increases the antibody response to sheep red blood cells, and activates natural killer cell activity against Yac-1 lymphoma cells in murine splenocyte cultures (EC50s = 10-50, 3-20, and 13-22 μM, respectively).{42514} Loxoribine (250 μM) increases production of IL-12, IL-23, IL-27, and IL-10 by human monocyte-derived dendritic cells (MoDCs).{42516} Loxoribine-treated MoDCs induce higher levels of IL-17 and IFN-γ secretion by co-cultured allogeneic CD4+ T cells compared to control MoDCs. Loxoribine (120 mg/kg) reduces the number of pulmonary metastases in the B16 mouse model of melanoma, an effect enhanced by co-administration of IL-2, and exhibits adjuvant activity in mice immunized with a B16 tumor vaccine.{42517}
Brand:CaymanSKU:21186 -Out of stock
Loxoribine is a guanosine derivative and an agonist of toll-like receptor 7 (TLR7).{42514,42515} It is selective for TLR7 over other human TLRs in a cell-based reporter assay at 1 mM.{42515}. Loxoribine induces proliferation, increases the antibody response to sheep red blood cells, and activates natural killer cell activity against Yac-1 lymphoma cells in murine splenocyte cultures (EC50s = 10-50, 3-20, and 13-22 μM, respectively).{42514} Loxoribine (250 μM) increases production of IL-12, IL-23, IL-27, and IL-10 by human monocyte-derived dendritic cells (MoDCs).{42516} Loxoribine-treated MoDCs induce higher levels of IL-17 and IFN-γ secretion by co-cultured allogeneic CD4+ T cells compared to control MoDCs. Loxoribine (120 mg/kg) reduces the number of pulmonary metastases in the B16 mouse model of melanoma, an effect enhanced by co-administration of IL-2, and exhibits adjuvant activity in mice immunized with a B16 tumor vaccine.{42517}
Brand:CaymanSKU:21186 -Out of stock
Loxoribine is a guanosine derivative and an agonist of toll-like receptor 7 (TLR7).{42514,42515} It is selective for TLR7 over other human TLRs in a cell-based reporter assay at 1 mM.{42515}. Loxoribine induces proliferation, increases the antibody response to sheep red blood cells, and activates natural killer cell activity against Yac-1 lymphoma cells in murine splenocyte cultures (EC50s = 10-50, 3-20, and 13-22 μM, respectively).{42514} Loxoribine (250 μM) increases production of IL-12, IL-23, IL-27, and IL-10 by human monocyte-derived dendritic cells (MoDCs).{42516} Loxoribine-treated MoDCs induce higher levels of IL-17 and IFN-γ secretion by co-cultured allogeneic CD4+ T cells compared to control MoDCs. Loxoribine (120 mg/kg) reduces the number of pulmonary metastases in the B16 mouse model of melanoma, an effect enhanced by co-administration of IL-2, and exhibits adjuvant activity in mice immunized with a B16 tumor vaccine.{42517}
Brand:CaymanSKU:21186 -Out of stock
LP-211 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.58 nM).{48788} It is selective for 5-HT7 over 5-HT1A and dopamine D2 receptors (Kis = 188 and 142 nM, respectively). It induces relaxation of isolated guinea pig ileum precontracted by substance P (Item No. 24035; EC50 = 0.6 μM). LP-211 (100 nM) stimulates neurite outgrowth in primary murine striatal and cortical neurons.{48789}
Brand:CaymanSKU:29659 - 10 mgAvailable on backorder
LP-211 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.58 nM).{48788} It is selective for 5-HT7 over 5-HT1A and dopamine D2 receptors (Kis = 188 and 142 nM, respectively). It induces relaxation of isolated guinea pig ileum precontracted by substance P (Item No. 24035; EC50 = 0.6 μM). LP-211 (100 nM) stimulates neurite outgrowth in primary murine striatal and cortical neurons.{48789}
Brand:CaymanSKU:29659 - 25 mgAvailable on backorder
LP-211 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.58 nM).{48788} It is selective for 5-HT7 over 5-HT1A and dopamine D2 receptors (Kis = 188 and 142 nM, respectively). It induces relaxation of isolated guinea pig ileum precontracted by substance P (Item No. 24035; EC50 = 0.6 μM). LP-211 (100 nM) stimulates neurite outgrowth in primary murine striatal and cortical neurons.{48789}
Brand:CaymanSKU:29659 - 5 mgAvailable on backorder
LP-211 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.58 nM).{48788} It is selective for 5-HT7 over 5-HT1A and dopamine D2 receptors (Kis = 188 and 142 nM, respectively). It induces relaxation of isolated guinea pig ileum precontracted by substance P (Item No. 24035; EC50 = 0.6 μM). LP-211 (100 nM) stimulates neurite outgrowth in primary murine striatal and cortical neurons.{48789}
Brand:CaymanSKU:29659 - 50 mgAvailable on backorder
LP-533401 is an inhibitor of tryptophan 5-hydroxylase 1 (Tph1) that blocks the biosynthesis of gut-derived serotonin, completely inhibiting serotonin production in Tph1-expressing cells at a dose of 1 µM.{32686} It prevents the development of and fully rescues, in a dose-dependent manner, osteoporosis in ovariectomized and aged mice.{32686,32684} LP-533401 has also been used to elucidate the role of gut-derived serotonin in pulmonary hypertension and leukemia in mice.{32683,32685}
Brand:CaymanSKU:10492 - 1 mgAvailable on backorder
LP-533401 is an inhibitor of tryptophan 5-hydroxylase 1 (Tph1) that blocks the biosynthesis of gut-derived serotonin, completely inhibiting serotonin production in Tph1-expressing cells at a dose of 1 µM.{32686} It prevents the development of and fully rescues, in a dose-dependent manner, osteoporosis in ovariectomized and aged mice.{32686,32684} LP-533401 has also been used to elucidate the role of gut-derived serotonin in pulmonary hypertension and leukemia in mice.{32683,32685}
Brand:CaymanSKU:10492 - 10 mgAvailable on backorder
LP-533401 is an inhibitor of tryptophan 5-hydroxylase 1 (Tph1) that blocks the biosynthesis of gut-derived serotonin, completely inhibiting serotonin production in Tph1-expressing cells at a dose of 1 µM.{32686} It prevents the development of and fully rescues, in a dose-dependent manner, osteoporosis in ovariectomized and aged mice.{32686,32684} LP-533401 has also been used to elucidate the role of gut-derived serotonin in pulmonary hypertension and leukemia in mice.{32683,32685}
Brand:CaymanSKU:10492 - 25 mgAvailable on backorder
LP-533401 is an inhibitor of tryptophan 5-hydroxylase 1 (Tph1) that blocks the biosynthesis of gut-derived serotonin, completely inhibiting serotonin production in Tph1-expressing cells at a dose of 1 µM.{32686} It prevents the development of and fully rescues, in a dose-dependent manner, osteoporosis in ovariectomized and aged mice.{32686,32684} LP-533401 has also been used to elucidate the role of gut-derived serotonin in pulmonary hypertension and leukemia in mice.{32683,32685}
Brand:CaymanSKU:10492 - 5 mgAvailable on backorder
LP44 is a full agonist of the serotonin 5-HT7 receptor (Ki = 0.22 nM) that displays 200- and greater than 1,000-fold selectivity over 5-HT1A (Ki = 52.7 nM) and 5-HT2A (Ki = 326 nM) receptors, respectively.{28320} It can induce relaxation of substance P-induced guinea pig ileum contraction with an EC50 value of 2.56 μM.{28320}
Brand:CaymanSKU:-Available on backorder
LP44 is a full agonist of the serotonin 5-HT7 receptor (Ki = 0.22 nM) that displays 200- and greater than 1,000-fold selectivity over 5-HT1A (Ki = 52.7 nM) and 5-HT2A (Ki = 326 nM) receptors, respectively.{28320} It can induce relaxation of substance P-induced guinea pig ileum contraction with an EC50 value of 2.56 μM.{28320}
Brand:CaymanSKU:-Available on backorder
LP44 is a full agonist of the serotonin 5-HT7 receptor (Ki = 0.22 nM) that displays 200- and greater than 1,000-fold selectivity over 5-HT1A (Ki = 52.7 nM) and 5-HT2A (Ki = 326 nM) receptors, respectively.{28320} It can induce relaxation of substance P-induced guinea pig ileum contraction with an EC50 value of 2.56 μM.{28320}
Brand:CaymanSKU:-Available on backorder
LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry.{38168,31210} It is selective for BRD7/9 over a panel of 48 BRDs at concentrations up to 10 µM determined using differential scanning fluorimetry. It inhibits BRD7 interactions with histones H3.3 and H4 with IC50 values of 3.7 and 3.3 µM, respectively, in a bioluminescence resonance energy transfer (BRET) assay in HEK293 cells. Similarly, it inhibits BRD9 from interacting with H3.3 and H4 with IC50 values of 5.1 and 6.2 µM, respectively. It also decreases the level of IL-6 secreted from LPS-stimulated THP-1 cells. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry.{38168,31210} It is selective for BRD7/9 over a panel of 48 BRDs at concentrations up to 10 µM determined using differential scanning fluorimetry. It inhibits BRD7 interactions with histones H3.3 and H4 with IC50 values of 3.7 and 3.3 µM, respectively, in a bioluminescence resonance energy transfer (BRET) assay in HEK293 cells. Similarly, it inhibits BRD9 from interacting with H3.3 and H4 with IC50 values of 5.1 and 6.2 µM, respectively. It also decreases the level of IL-6 secreted from LPS-stimulated THP-1 cells. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry.{38168,31210} It is selective for BRD7/9 over a panel of 48 BRDs at concentrations up to 10 µM determined using differential scanning fluorimetry. It inhibits BRD7 interactions with histones H3.3 and H4 with IC50 values of 3.7 and 3.3 µM, respectively, in a bioluminescence resonance energy transfer (BRET) assay in HEK293 cells. Similarly, it inhibits BRD9 from interacting with H3.3 and H4 with IC50 values of 5.1 and 6.2 µM, respectively. It also decreases the level of IL-6 secreted from LPS-stimulated THP-1 cells. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Available on backorder
LPA2 antagonist 1 is an antagonist of lysophosphatidic acid receptor 2 (LPA2; IC50 = 17 nM).{43178} It is selective for LPA2 over LPA1 and LPA3 (IC50s = >50 μM). LPA2 antagonist 1 inhibits HGF-induced phosphorylation of ERK and proliferation of HCT116 colon cancer cells in a concentration-dependent manner.
Brand:CaymanSKU:22051 -Out of stock
LPA2 antagonist 1 is an antagonist of lysophosphatidic acid receptor 2 (LPA2; IC50 = 17 nM).{43178} It is selective for LPA2 over LPA1 and LPA3 (IC50s = >50 μM). LPA2 antagonist 1 inhibits HGF-induced phosphorylation of ERK and proliferation of HCT116 colon cancer cells in a concentration-dependent manner.
Brand:CaymanSKU:22051 -Out of stock
LPA2 antagonist 1 is an antagonist of lysophosphatidic acid receptor 2 (LPA2; IC50 = 17 nM).{43178} It is selective for LPA2 over LPA1 and LPA3 (IC50s = >50 μM). LPA2 antagonist 1 inhibits HGF-induced phosphorylation of ERK and proliferation of HCT116 colon cancer cells in a concentration-dependent manner.
Brand:CaymanSKU:22051 -Out of stock
Brand:CaymanSKU:705018 - 1 eaAvailable on backorder
Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson’s disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. LRRK2-IN-1 is a potent inhibitor of LRRK2 that inhibits both wild-type and G2019S mutant LRRK2 (IC50s = 13 and 6 nM, respectively).{29460} It is selective for LRRK2 over a large panel of other kinases. LRRK2-IN-1 treatment causes dephosphorylation of LRRK2, leading to its dissociation from 14-3-3 proteins, ubiquitination, and degradation.{29460,29462} Inhibitors of LRRK2, including LRRK2-IN-1, stimulate macroautophagy in H4 neuroglioma cells.{29461}
Brand:CaymanSKU:-Available on backorder
Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson’s disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. LRRK2-IN-1 is a potent inhibitor of LRRK2 that inhibits both wild-type and G2019S mutant LRRK2 (IC50s = 13 and 6 nM, respectively).{29460} It is selective for LRRK2 over a large panel of other kinases. LRRK2-IN-1 treatment causes dephosphorylation of LRRK2, leading to its dissociation from 14-3-3 proteins, ubiquitination, and degradation.{29460,29462} Inhibitors of LRRK2, including LRRK2-IN-1, stimulate macroautophagy in H4 neuroglioma cells.{29461}
Brand:CaymanSKU:-Available on backorder
Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson’s disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. LRRK2-IN-1 is a potent inhibitor of LRRK2 that inhibits both wild-type and G2019S mutant LRRK2 (IC50s = 13 and 6 nM, respectively).{29460} It is selective for LRRK2 over a large panel of other kinases. LRRK2-IN-1 treatment causes dephosphorylation of LRRK2, leading to its dissociation from 14-3-3 proteins, ubiquitination, and degradation.{29460,29462} Inhibitors of LRRK2, including LRRK2-IN-1, stimulate macroautophagy in H4 neuroglioma cells.{29461}
Brand:CaymanSKU:-Available on backorder
LSN2463359 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5; EC50 = 24 nM).{34519} It is without effect at other mGluRs. LSN2463359 is brain penetrant and reverses learning deficits in a rat model of schizophrenia.{34519,34521} Through its effects on mGluR5, LSN2463359 attenuates deficits in performance in operant behavior induced by SDZ-220581, an NMDA (Item No. 14581) receptor antagonist, in rats.{34520,34521} It also promotes wakefulness in animals.{34521}
Brand:CaymanSKU:22104 -Out of stock
LSN2463359 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5; EC50 = 24 nM).{34519} It is without effect at other mGluRs. LSN2463359 is brain penetrant and reverses learning deficits in a rat model of schizophrenia.{34519,34521} Through its effects on mGluR5, LSN2463359 attenuates deficits in performance in operant behavior induced by SDZ-220581, an NMDA (Item No. 14581) receptor antagonist, in rats.{34520,34521} It also promotes wakefulness in animals.{34521}
Brand:CaymanSKU:22104 -Out of stock
LSN2463359 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5; EC50 = 24 nM).{34519} It is without effect at other mGluRs. LSN2463359 is brain penetrant and reverses learning deficits in a rat model of schizophrenia.{34519,34521} Through its effects on mGluR5, LSN2463359 attenuates deficits in performance in operant behavior induced by SDZ-220581, an NMDA (Item No. 14581) receptor antagonist, in rats.{34520,34521} It also promotes wakefulness in animals.{34521}
Brand:CaymanSKU:22104 -Out of stock
LSN2463359 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5; EC50 = 24 nM).{34519} It is without effect at other mGluRs. LSN2463359 is brain penetrant and reverses learning deficits in a rat model of schizophrenia.{34519,34521} Through its effects on mGluR5, LSN2463359 attenuates deficits in performance in operant behavior induced by SDZ-220581, an NMDA (Item No. 14581) receptor antagonist, in rats.{34520,34521} It also promotes wakefulness in animals.{34521}
Brand:CaymanSKU:22104 -Out of stock
Peroxisome proliferator-activated receptors (PPARs) are activated by fatty acids and eicosanoids as well as antidyslipidemic agents. Among the receptor isotypes, PPARα demonstrates a particular role in fatty acid oxidation whereas PPARγ is known to be involved in adipocyte differentiation and lipid storage. LT175 is a dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC50s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively).{28659} It exhibits low adipogenic activity in vitro and improves glucose homeostasis in diet-induced insulin resistant mice.{28659} LT175 was shown to disrupt the recruitment of coregulators, cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1, to PPARγ.{28659}
Brand:CaymanSKU:-Available on backorder
Peroxisome proliferator-activated receptors (PPARs) are activated by fatty acids and eicosanoids as well as antidyslipidemic agents. Among the receptor isotypes, PPARα demonstrates a particular role in fatty acid oxidation whereas PPARγ is known to be involved in adipocyte differentiation and lipid storage. LT175 is a dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC50s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively).{28659} It exhibits low adipogenic activity in vitro and improves glucose homeostasis in diet-induced insulin resistant mice.{28659} LT175 was shown to disrupt the recruitment of coregulators, cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1, to PPARγ.{28659}
Brand:CaymanSKU:-Available on backorder
Peroxisome proliferator-activated receptors (PPARs) are activated by fatty acids and eicosanoids as well as antidyslipidemic agents. Among the receptor isotypes, PPARα demonstrates a particular role in fatty acid oxidation whereas PPARγ is known to be involved in adipocyte differentiation and lipid storage. LT175 is a dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC50s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively).{28659} It exhibits low adipogenic activity in vitro and improves glucose homeostasis in diet-induced insulin resistant mice.{28659} LT175 was shown to disrupt the recruitment of coregulators, cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1, to PPARγ.{28659}
Brand:CaymanSKU:-Available on backorder
Peroxisome proliferator-activated receptors (PPARs) are activated by fatty acids and eicosanoids as well as antidyslipidemic agents. Among the receptor isotypes, PPARα demonstrates a particular role in fatty acid oxidation whereas PPARγ is known to be involved in adipocyte differentiation and lipid storage. LT175 is a dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC50s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively).{28659} It exhibits low adipogenic activity in vitro and improves glucose homeostasis in diet-induced insulin resistant mice.{28659} LT175 was shown to disrupt the recruitment of coregulators, cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1, to PPARγ.{28659}
Brand:CaymanSKU:-Available on backorder
LU AE58054 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.83 nM).{48420} It is selective for 5-HT6 over other 5-HT receptor subtypes (Kis = 250 to >10,000 nM) and 70 other targets but does bind to α1A- and α1B-adrenergic receptors (α1B-ARs; Kis = 21 and 22 nM, respectively). LU AE58054 (5-20 mg/kg) reverses phencyclidine-induced deficits in novel object recognition memory in rats. When administered in combination with the cholinesterase inhibitor rivastigmine (Item No. 14270), LU AE58054 has an additive effect on the decreased number of slips and falls made by rats with bilateral striatal-dopaminergic and cortical-cholinergic system lesions, a model of Parkinson’s disease motor disruption, in the Michigan complex motor control task.{48421}
Brand:CaymanSKU:27335 - 100 mgAvailable on backorder
LU AE58054 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.83 nM).{48420} It is selective for 5-HT6 over other 5-HT receptor subtypes (Kis = 250 to >10,000 nM) and 70 other targets but does bind to α1A- and α1B-adrenergic receptors (α1B-ARs; Kis = 21 and 22 nM, respectively). LU AE58054 (5-20 mg/kg) reverses phencyclidine-induced deficits in novel object recognition memory in rats. When administered in combination with the cholinesterase inhibitor rivastigmine (Item No. 14270), LU AE58054 has an additive effect on the decreased number of slips and falls made by rats with bilateral striatal-dopaminergic and cortical-cholinergic system lesions, a model of Parkinson’s disease motor disruption, in the Michigan complex motor control task.{48421}
Brand:CaymanSKU:27335 - 25 mgAvailable on backorder
LU AE58054 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.83 nM).{48420} It is selective for 5-HT6 over other 5-HT receptor subtypes (Kis = 250 to >10,000 nM) and 70 other targets but does bind to α1A- and α1B-adrenergic receptors (α1B-ARs; Kis = 21 and 22 nM, respectively). LU AE58054 (5-20 mg/kg) reverses phencyclidine-induced deficits in novel object recognition memory in rats. When administered in combination with the cholinesterase inhibitor rivastigmine (Item No. 14270), LU AE58054 has an additive effect on the decreased number of slips and falls made by rats with bilateral striatal-dopaminergic and cortical-cholinergic system lesions, a model of Parkinson’s disease motor disruption, in the Michigan complex motor control task.{48421}
Brand:CaymanSKU:27335 - 250 mgAvailable on backorder
LU AE58054 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.83 nM).{48420} It is selective for 5-HT6 over other 5-HT receptor subtypes (Kis = 250 to >10,000 nM) and 70 other targets but does bind to α1A- and α1B-adrenergic receptors (α1B-ARs; Kis = 21 and 22 nM, respectively). LU AE58054 (5-20 mg/kg) reverses phencyclidine-induced deficits in novel object recognition memory in rats. When administered in combination with the cholinesterase inhibitor rivastigmine (Item No. 14270), LU AE58054 has an additive effect on the decreased number of slips and falls made by rats with bilateral striatal-dopaminergic and cortical-cholinergic system lesions, a model of Parkinson’s disease motor disruption, in the Michigan complex motor control task.{48421}
Brand:CaymanSKU:27335 - 50 mgAvailable on backorder
Lu AF21934 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 4 (mGluR4; EC50 = 500 nM for the human receptor in a FLIPR assay).{48374} It is selective for mGluR4 over mGluR6 (EC50 = 7 μM) and a panel of 73 CNS ion channels, G protein-coupled receptors (GPCRs), and enzymes at 10 μM. Lu AF21934 (12 mg/kg) reduces marble burying behavior and stress-induced hyperthermia in mice, indicating anxiolytic-like activity, but also reduces locomotor activity. It inhibits MK-801- and amphetamine-induced hyperactivity in mice and prevents MK-801-induced decreases in social interaction in rats.{48375} Lu AF21934 (0.5 and 2.5 mg/kg) also reduces harmaline-induced hyperactivity, but not tremor, in rats.{48376}
Brand:CaymanSKU:27045 - 1 mgAvailable on backorder
Lu AF21934 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 4 (mGluR4; EC50 = 500 nM for the human receptor in a FLIPR assay).{48374} It is selective for mGluR4 over mGluR6 (EC50 = 7 μM) and a panel of 73 CNS ion channels, G protein-coupled receptors (GPCRs), and enzymes at 10 μM. Lu AF21934 (12 mg/kg) reduces marble burying behavior and stress-induced hyperthermia in mice, indicating anxiolytic-like activity, but also reduces locomotor activity. It inhibits MK-801- and amphetamine-induced hyperactivity in mice and prevents MK-801-induced decreases in social interaction in rats.{48375} Lu AF21934 (0.5 and 2.5 mg/kg) also reduces harmaline-induced hyperactivity, but not tremor, in rats.{48376}
Brand:CaymanSKU:27045 - 10 mgAvailable on backorder
Lu AF21934 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 4 (mGluR4; EC50 = 500 nM for the human receptor in a FLIPR assay).{48374} It is selective for mGluR4 over mGluR6 (EC50 = 7 μM) and a panel of 73 CNS ion channels, G protein-coupled receptors (GPCRs), and enzymes at 10 μM. Lu AF21934 (12 mg/kg) reduces marble burying behavior and stress-induced hyperthermia in mice, indicating anxiolytic-like activity, but also reduces locomotor activity. It inhibits MK-801- and amphetamine-induced hyperactivity in mice and prevents MK-801-induced decreases in social interaction in rats.{48375} Lu AF21934 (0.5 and 2.5 mg/kg) also reduces harmaline-induced hyperactivity, but not tremor, in rats.{48376}
Brand:CaymanSKU:27045 - 25 mgAvailable on backorder
Lu AF21934 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 4 (mGluR4; EC50 = 500 nM for the human receptor in a FLIPR assay).{48374} It is selective for mGluR4 over mGluR6 (EC50 = 7 μM) and a panel of 73 CNS ion channels, G protein-coupled receptors (GPCRs), and enzymes at 10 μM. Lu AF21934 (12 mg/kg) reduces marble burying behavior and stress-induced hyperthermia in mice, indicating anxiolytic-like activity, but also reduces locomotor activity. It inhibits MK-801- and amphetamine-induced hyperactivity in mice and prevents MK-801-induced decreases in social interaction in rats.{48375} Lu AF21934 (0.5 and 2.5 mg/kg) also reduces harmaline-induced hyperactivity, but not tremor, in rats.{48376}
Brand:CaymanSKU:27045 - 5 mgAvailable on backorder
Lucidenic acid A is a triterpene originally isolated from G. lucidum and has anticancer activity.{52479,52480} It is cytotoxic to HepG2, HepG2/2.15, and P388 cancer cells (IC50s = 0.164, 0.205, and 17 nM, respectively). Lucidenic acid A inhibits increases in matrix metalloproteinase-2 (MMP-2) and MMP-9 activity and Matrigel™ invasion induced by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) in HepG2 cells.{52480}
Brand:CaymanSKU:30372 - 1 mgAvailable on backorder
Lucidenic acid A is a triterpene originally isolated from G. lucidum and has anticancer activity.{52479,52480} It is cytotoxic to HepG2, HepG2/2.15, and P388 cancer cells (IC50s = 0.164, 0.205, and 17 nM, respectively). Lucidenic acid A inhibits increases in matrix metalloproteinase-2 (MMP-2) and MMP-9 activity and Matrigel™ invasion induced by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) in HepG2 cells.{52480}
Brand:CaymanSKU:30372 - 10 mgAvailable on backorder