Chemicals
Showing 20701–20850 of 41137 results
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GIT 27 is an orally active, isoxazole compound that exhibits various immunomodulatory properties both in vitro and in preclinical in vivo models of autoimmune diseases by inhibiting inflammatory antigen presentation.{30814} It has been shown to target macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, macrophage migration inhibitory factor, and inducible nitric oxide synthase-mediated nitric oxide generation in both pancreatic islets and peripheral compartments.{30815} GIT 27 can also prevent IL-1β/interferon-γ-induced pancreatic islet death in vitro at 10 µg/ml and reduce the cumulative incidence of diabetes and insulitis in a mouse model of type 1 diabetes at 20 mg/kg.{30815}
Brand:CaymanSKU:- GIT 27 is an orally active, isoxazole compound that exhibits various immunomodulatory properties both in vitro and in preclinical in vivo models of autoimmune diseases by inhibiting inflammatory antigen presentation.{30814} It has been shown to target macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, macrophage migration inhibitory factor, and inducible nitric oxide synthase-mediated nitric oxide generation in both pancreatic islets and peripheral compartments.{30815} GIT 27 can also prevent IL-1β/interferon-γ-induced pancreatic islet death in vitro at 10 µg/ml and reduce the cumulative incidence of diabetes and insulitis in a mouse model of type 1 diabetes at 20 mg/kg.{30815}
Brand:CaymanSKU:- GIT 27 is an orally active, isoxazole compound that exhibits various immunomodulatory properties both in vitro and in preclinical in vivo models of autoimmune diseases by inhibiting inflammatory antigen presentation.{30814} It has been shown to target macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, macrophage migration inhibitory factor, and inducible nitric oxide synthase-mediated nitric oxide generation in both pancreatic islets and peripheral compartments.{30815} GIT 27 can also prevent IL-1β/interferon-γ-induced pancreatic islet death in vitro at 10 µg/ml and reduce the cumulative incidence of diabetes and insulitis in a mouse model of type 1 diabetes at 20 mg/kg.{30815}
Brand:CaymanSKU:- GIT 27 is an orally active, isoxazole compound that exhibits various immunomodulatory properties both in vitro and in preclinical in vivo models of autoimmune diseases by inhibiting inflammatory antigen presentation.{30814} It has been shown to target macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, macrophage migration inhibitory factor, and inducible nitric oxide synthase-mediated nitric oxide generation in both pancreatic islets and peripheral compartments.{30815} GIT 27 can also prevent IL-1β/interferon-γ-induced pancreatic islet death in vitro at 10 µg/ml and reduce the cumulative incidence of diabetes and insulitis in a mouse model of type 1 diabetes at 20 mg/kg.{30815}
Brand:CaymanSKU:-Out of stock
GJ-103 is an inducer of stop codon read-through.{46443} It restores the kinase activity of ataxia-telangiectasia mutated kinase (ATM) in patient-derived ataxia telangiectasia (A-T) lymphoblastoid cell lines containing homozygous TAG, TGA, or TAA nonsense mutations in ATM when used at concentrations of 10 and 30 μM.
Brand:CaymanSKU:22482 -Out of stock
GJ-103 is an inducer of stop codon read-through.{46443} It restores the kinase activity of ataxia-telangiectasia mutated kinase (ATM) in patient-derived ataxia telangiectasia (A-T) lymphoblastoid cell lines containing homozygous TAG, TGA, or TAA nonsense mutations in ATM when used at concentrations of 10 and 30 μM.
Brand:CaymanSKU:22482 -Out of stock
GJ-103 is an inducer of stop codon read-through.{46443} It restores the kinase activity of ataxia-telangiectasia mutated kinase (ATM) in patient-derived ataxia telangiectasia (A-T) lymphoblastoid cell lines containing homozygous TAG, TGA, or TAA nonsense mutations in ATM when used at concentrations of 10 and 30 μM.
Brand:CaymanSKU:22482 -Out of stock
GJ-103 is an inducer of stop codon read-through.{46443} It restores the kinase activity of ataxia-telangiectasia mutated kinase (ATM) in patient-derived ataxia telangiectasia (A-T) lymphoblastoid cell lines containing homozygous TAG, TGA, or TAA nonsense mutations in ATM when used at concentrations of 10 and 30 μM.
Brand:CaymanSKU:22482 -Out of stock
GK187 is an inhibitor of Group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2), an enzyme involved in basal cell metabolism.{40941} It inhibits GVIA iPLA2 by 99.8% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows less than 25% and 32.8% inhibition, respectively.
Brand:CaymanSKU:25130 - 1 mgAvailable on backorder
GK187 is an inhibitor of Group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2), an enzyme involved in basal cell metabolism.{40941} It inhibits GVIA iPLA2 by 99.8% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows less than 25% and 32.8% inhibition, respectively.
Brand:CaymanSKU:25130 - 10 mgAvailable on backorder
GK187 is an inhibitor of Group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2), an enzyme involved in basal cell metabolism.{40941} It inhibits GVIA iPLA2 by 99.8% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows less than 25% and 32.8% inhibition, respectively.
Brand:CaymanSKU:25130 - 5 mgAvailable on backorder
GK187 is an inhibitor of Group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2), an enzyme involved in basal cell metabolism.{40941} It inhibits GVIA iPLA2 by 99.8% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows less than 25% and 32.8% inhibition, respectively.
Brand:CaymanSKU:25130 - 500 µgAvailable on backorder
GKK1032B is a fungal metabolite originally isolated from Penicillium sp. GKK1032 that has antiproliferative and antibacterial activities.{48590,48591} GKK1032B inhibits the growth of HeLa S3 cervical and MCF-7 breast cancer cells (IC50s = 17.7 and 14.71 μM, respectively) and Vero cells (IC50 = 29.55 μM). It also inhibits the growth of B. subtilis (MIC = 20.8 μg/ml) and M. tuberculosis (MIC = 48.35 μM).
Brand:CaymanSKU:28855 - 1 mgAvailable on backorder
NADPH oxidase 1 (NOX1) and NOX4 generate reactive oxygen species (ROS) that are critical in regulating a variety of cellular functions but also contribute to many diseases.{28976,28981} GKT137831 is a dual inhibitor of both NOX1 and NOX4 with Ki values in the range of 100 to 150 nM in cell-free assays of ROS production.{28980} It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.{28980,28982} GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.{28980,28982,28975} It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.{28978,28977,28979}
Brand:CaymanSKU:-Available on backorder
NADPH oxidase 1 (NOX1) and NOX4 generate reactive oxygen species (ROS) that are critical in regulating a variety of cellular functions but also contribute to many diseases.{28976,28981} GKT137831 is a dual inhibitor of both NOX1 and NOX4 with Ki values in the range of 100 to 150 nM in cell-free assays of ROS production.{28980} It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.{28980,28982} GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.{28980,28982,28975} It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.{28978,28977,28979}
Brand:CaymanSKU:-Available on backorder
NADPH oxidase 1 (NOX1) and NOX4 generate reactive oxygen species (ROS) that are critical in regulating a variety of cellular functions but also contribute to many diseases.{28976,28981} GKT137831 is a dual inhibitor of both NOX1 and NOX4 with Ki values in the range of 100 to 150 nM in cell-free assays of ROS production.{28980} It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.{28980,28982} GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.{28980,28982,28975} It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.{28978,28977,28979}
Brand:CaymanSKU:-Available on backorder
NADPH oxidase 1 (NOX1) and NOX4 generate reactive oxygen species (ROS) that are critical in regulating a variety of cellular functions but also contribute to many diseases.{28976,28981} GKT137831 is a dual inhibitor of both NOX1 and NOX4 with Ki values in the range of 100 to 150 nM in cell-free assays of ROS production.{28980} It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.{28980,28982} GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.{28980,28982,28975} It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.{28978,28977,28979}
Brand:CaymanSKU:-Available on backorder
Glabridin is a prenylated isoflavonoid found in licorice root extract that is reported to possess antiviral, antimicrobial, anti-inflammatory, antidiabetic, antiatherogenic, antioxidant, antitumor, and estrogen-like properties.{31662,31661,30137} These diverse biological activities are largely related to the capacity of glabridin to down-regulate reactive oxygen species, bind to antioxidant effectors, and act as a selective estrogen receptor modulator.{33359}
Brand:CaymanSKU:11843 - 10 mgAvailable on backorder
Glabridin is a prenylated isoflavonoid found in licorice root extract that is reported to possess antiviral, antimicrobial, anti-inflammatory, antidiabetic, antiatherogenic, antioxidant, antitumor, and estrogen-like properties.{31662,31661,30137} These diverse biological activities are largely related to the capacity of glabridin to down-regulate reactive oxygen species, bind to antioxidant effectors, and act as a selective estrogen receptor modulator.{33359}
Brand:CaymanSKU:11843 - 25 mgAvailable on backorder
Glabridin is a prenylated isoflavonoid found in licorice root extract that is reported to possess antiviral, antimicrobial, anti-inflammatory, antidiabetic, antiatherogenic, antioxidant, antitumor, and estrogen-like properties.{31662,31661,30137} These diverse biological activities are largely related to the capacity of glabridin to down-regulate reactive oxygen species, bind to antioxidant effectors, and act as a selective estrogen receptor modulator.{33359}
Brand:CaymanSKU:11843 - 5 mgAvailable on backorder
Glabridin is a prenylated isoflavonoid found in licorice root extract that is reported to possess antiviral, antimicrobial, anti-inflammatory, antidiabetic, antiatherogenic, antioxidant, antitumor, and estrogen-like properties.{31662,31661,30137} These diverse biological activities are largely related to the capacity of glabridin to down-regulate reactive oxygen species, bind to antioxidant effectors, and act as a selective estrogen receptor modulator.{33359}
Brand:CaymanSKU:11843 - 50 mgAvailable on backorder
Glatiramer (acetate) is a mixture of synthetic polypeptides composed of four amino acids found in myelin basic protein (MBP): L-Alanine, L-glutamic acid, L-lysine, and L-tyrosine. It prevents MBP from binding to MHC class II molecules in the periphery and induces the production of immunomodulatory molecules considered to be anti-inflammatory.{33964} It also increases proliferation of oligodendrocyte and neuronal precursor cells in the central nervous system of mice.{33965,33963} Formulations containing glatiramer (acetate) are used to treat patients with multiple sclerosis, particularly the relapsing-remitting type.{33966}
Brand:CaymanSKU:9000571 - 1 mgAvailable on backorder
Glatiramer (acetate) is a mixture of synthetic polypeptides composed of four amino acids found in myelin basic protein (MBP): L-Alanine, L-glutamic acid, L-lysine, and L-tyrosine. It prevents MBP from binding to MHC class II molecules in the periphery and induces the production of immunomodulatory molecules considered to be anti-inflammatory.{33964} It also increases proliferation of oligodendrocyte and neuronal precursor cells in the central nervous system of mice.{33965,33963} Formulations containing glatiramer (acetate) are used to treat patients with multiple sclerosis, particularly the relapsing-remitting type.{33966}
Brand:CaymanSKU:9000571 - 10 mgAvailable on backorder
Glatiramer (acetate) is a mixture of synthetic polypeptides composed of four amino acids found in myelin basic protein (MBP): L-Alanine, L-glutamic acid, L-lysine, and L-tyrosine. It prevents MBP from binding to MHC class II molecules in the periphery and induces the production of immunomodulatory molecules considered to be anti-inflammatory.{33964} It also increases proliferation of oligodendrocyte and neuronal precursor cells in the central nervous system of mice.{33965,33963} Formulations containing glatiramer (acetate) are used to treat patients with multiple sclerosis, particularly the relapsing-remitting type.{33966}
Brand:CaymanSKU:9000571 - 25 mgAvailable on backorder
Glatiramer (acetate) is a mixture of synthetic polypeptides composed of four amino acids found in myelin basic protein (MBP): L-Alanine, L-glutamic acid, L-lysine, and L-tyrosine. It prevents MBP from binding to MHC class II molecules in the periphery and induces the production of immunomodulatory molecules considered to be anti-inflammatory.{33964} It also increases proliferation of oligodendrocyte and neuronal precursor cells in the central nervous system of mice.{33965,33963} Formulations containing glatiramer (acetate) are used to treat patients with multiple sclerosis, particularly the relapsing-remitting type.{33966}
Brand:CaymanSKU:9000571 - 5 mgAvailable on backorder
Glaucine is an alkaloid originally isolated from G. flavum that demonstrates antitussive properties.{28311} It is structurally related to papaverine (Item No. 10011133), a non-selective phosphodiesterase (PDE) inhibitor. Glaucine selectively inhibits PDE4 (Kis = 3.4 µM in human bronchus and polymorphonuclear leukocytes).{28311} It has been shown to have bronchodilation and anti-inflammatory effects, inhibiting the spontaneous and histamine-induced tone in human isolated bronchus and augmenting cyclic AMP accumulation.{28311} Glaucine also binds to the benzothiazepine site on L-type Ca2+-channels in smooth muscle, blocking calcium ion signaling.{28311} This compound has been detected as a recreational drug capable of eliciting dissociative effects.{20293}
Brand:CaymanSKU:-Available on backorder
Glaucine is an alkaloid originally isolated from G. flavum that demonstrates antitussive properties.{28311} It is structurally related to papaverine (Item No. 10011133), a non-selective phosphodiesterase (PDE) inhibitor. Glaucine selectively inhibits PDE4 (Kis = 3.4 µM in human bronchus and polymorphonuclear leukocytes).{28311} It has been shown to have bronchodilation and anti-inflammatory effects, inhibiting the spontaneous and histamine-induced tone in human isolated bronchus and augmenting cyclic AMP accumulation.{28311} Glaucine also binds to the benzothiazepine site on L-type Ca2+-channels in smooth muscle, blocking calcium ion signaling.{28311} This compound has been detected as a recreational drug capable of eliciting dissociative effects.{20293}
Brand:CaymanSKU:-Available on backorder
Glaucine is an alkaloid originally isolated from G. flavum that demonstrates antitussive properties.{28311} It is structurally related to papaverine (Item No. 10011133), a non-selective phosphodiesterase (PDE) inhibitor. Glaucine selectively inhibits PDE4 (Kis = 3.4 µM in human bronchus and polymorphonuclear leukocytes).{28311} It has been shown to have bronchodilation and anti-inflammatory effects, inhibiting the spontaneous and histamine-induced tone in human isolated bronchus and augmenting cyclic AMP accumulation.{28311} Glaucine also binds to the benzothiazepine site on L-type Ca2+-channels in smooth muscle, blocking calcium ion signaling.{28311} This compound has been detected as a recreational drug capable of eliciting dissociative effects.{20293}
Brand:CaymanSKU:-Available on backorder
Glaucine is an alkaloid originally isolated from G. flavum that demonstrates antitussive properties.{28311} It is structurally related to papaverine (Item No. 10011133), a non-selective phosphodiesterase (PDE) inhibitor. Glaucine selectively inhibits PDE4 (Kis = 3.4 µM in human bronchus and polymorphonuclear leukocytes).{28311} It has been shown to have bronchodilation and anti-inflammatory effects, inhibiting the spontaneous and histamine-induced tone in human isolated bronchus and augmenting cyclic AMP accumulation.{28311} Glaucine also binds to the benzothiazepine site on L-type Ca2+-channels in smooth muscle, blocking calcium ion signaling.{28311} This compound has been detected as a recreational drug capable of eliciting dissociative effects.{20293}
Brand:CaymanSKU:-Available on backorder
Glecaprevir is an orally bioavailable and direct-acting inhibitor of the hepatitis C virus (HCV) non-structural 3/4A (NS3/4A) serine protease.{45435} It inhibits NS3/4A from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (IC50s = 4.6, 8.9, 3.5, 3.8, 7.9, 6.1, 8.1, and 11.3 nM, respectively) in cell-free assays but does not inhibit human chymase, chymotrypsin type II, chymotrypsin type VII, elastase, kallikrein, urokinase, or cathepsin B proteases (IC50s = >200,000 nM). Glecaprevir inhibits HCV replication in stable Huh7-derived replicon cells infected with subgenomic genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (EC50s = 0.85, 0.94, 2.2, 4.6, 1.9, 2.8, 1.4, and 0.86 nM, respectively). It also inhibits replication of clinical isolates of genotypes 1a (EC50s = 0.05-0.12 nM), 1b (EC50s = 0.20-0.68 nM), 2a (EC50s = 0.66-1.9 nM), 2b (EC50s = 1.4-3.2 nM), 3a (EC50s = 0.71-3.8 nM), and 4a (EC50s = 0.31-0.55 nM). Glecaprevir acts synergistically with the HCV NS5A protease inhibitor pibrentasvir (Item No. 27546) to inhibit HCV genotype 1b-Con1 replication in replicon cells. Formulations containing glecaprevir, in combination with pibrentasvir, have been used in the treatment of chronic HCV genotype 1, 2, 3, 4, 5, or 6 infection.
Brand:CaymanSKU:27934 - 1 mgAvailable on backorder
Glecaprevir is an orally bioavailable and direct-acting inhibitor of the hepatitis C virus (HCV) non-structural 3/4A (NS3/4A) serine protease.{45435} It inhibits NS3/4A from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (IC50s = 4.6, 8.9, 3.5, 3.8, 7.9, 6.1, 8.1, and 11.3 nM, respectively) in cell-free assays but does not inhibit human chymase, chymotrypsin type II, chymotrypsin type VII, elastase, kallikrein, urokinase, or cathepsin B proteases (IC50s = >200,000 nM). Glecaprevir inhibits HCV replication in stable Huh7-derived replicon cells infected with subgenomic genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (EC50s = 0.85, 0.94, 2.2, 4.6, 1.9, 2.8, 1.4, and 0.86 nM, respectively). It also inhibits replication of clinical isolates of genotypes 1a (EC50s = 0.05-0.12 nM), 1b (EC50s = 0.20-0.68 nM), 2a (EC50s = 0.66-1.9 nM), 2b (EC50s = 1.4-3.2 nM), 3a (EC50s = 0.71-3.8 nM), and 4a (EC50s = 0.31-0.55 nM). Glecaprevir acts synergistically with the HCV NS5A protease inhibitor pibrentasvir (Item No. 27546) to inhibit HCV genotype 1b-Con1 replication in replicon cells. Formulations containing glecaprevir, in combination with pibrentasvir, have been used in the treatment of chronic HCV genotype 1, 2, 3, 4, 5, or 6 infection.
Brand:CaymanSKU:27934 - 10 mgAvailable on backorder
Glecaprevir is an orally bioavailable and direct-acting inhibitor of the hepatitis C virus (HCV) non-structural 3/4A (NS3/4A) serine protease.{45435} It inhibits NS3/4A from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (IC50s = 4.6, 8.9, 3.5, 3.8, 7.9, 6.1, 8.1, and 11.3 nM, respectively) in cell-free assays but does not inhibit human chymase, chymotrypsin type II, chymotrypsin type VII, elastase, kallikrein, urokinase, or cathepsin B proteases (IC50s = >200,000 nM). Glecaprevir inhibits HCV replication in stable Huh7-derived replicon cells infected with subgenomic genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (EC50s = 0.85, 0.94, 2.2, 4.6, 1.9, 2.8, 1.4, and 0.86 nM, respectively). It also inhibits replication of clinical isolates of genotypes 1a (EC50s = 0.05-0.12 nM), 1b (EC50s = 0.20-0.68 nM), 2a (EC50s = 0.66-1.9 nM), 2b (EC50s = 1.4-3.2 nM), 3a (EC50s = 0.71-3.8 nM), and 4a (EC50s = 0.31-0.55 nM). Glecaprevir acts synergistically with the HCV NS5A protease inhibitor pibrentasvir (Item No. 27546) to inhibit HCV genotype 1b-Con1 replication in replicon cells. Formulations containing glecaprevir, in combination with pibrentasvir, have been used in the treatment of chronic HCV genotype 1, 2, 3, 4, 5, or 6 infection.
Brand:CaymanSKU:27934 - 25 mgAvailable on backorder
Glecaprevir is an orally bioavailable and direct-acting inhibitor of the hepatitis C virus (HCV) non-structural 3/4A (NS3/4A) serine protease.{45435} It inhibits NS3/4A from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (IC50s = 4.6, 8.9, 3.5, 3.8, 7.9, 6.1, 8.1, and 11.3 nM, respectively) in cell-free assays but does not inhibit human chymase, chymotrypsin type II, chymotrypsin type VII, elastase, kallikrein, urokinase, or cathepsin B proteases (IC50s = >200,000 nM). Glecaprevir inhibits HCV replication in stable Huh7-derived replicon cells infected with subgenomic genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a (EC50s = 0.85, 0.94, 2.2, 4.6, 1.9, 2.8, 1.4, and 0.86 nM, respectively). It also inhibits replication of clinical isolates of genotypes 1a (EC50s = 0.05-0.12 nM), 1b (EC50s = 0.20-0.68 nM), 2a (EC50s = 0.66-1.9 nM), 2b (EC50s = 1.4-3.2 nM), 3a (EC50s = 0.71-3.8 nM), and 4a (EC50s = 0.31-0.55 nM). Glecaprevir acts synergistically with the HCV NS5A protease inhibitor pibrentasvir (Item No. 27546) to inhibit HCV genotype 1b-Con1 replication in replicon cells. Formulations containing glecaprevir, in combination with pibrentasvir, have been used in the treatment of chronic HCV genotype 1, 2, 3, 4, 5, or 6 infection.
Brand:CaymanSKU:27934 - 5 mgAvailable on backorder
Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels (IC50 = 184 nM for murine β-cells).{47058,34125} It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 μM, respectively).{47058} Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide.{47059} Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels.{8975} It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ; Item No. 13104).{47060}
Brand:CaymanSKU:25503 - 1 gAvailable on backorder
Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels (IC50 = 184 nM for murine β-cells).{47058,34125} It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 μM, respectively).{47058} Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide.{47059} Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels.{8975} It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ; Item No. 13104).{47060}
Brand:CaymanSKU:25503 - 10 gAvailable on backorder
Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels (IC50 = 184 nM for murine β-cells).{47058,34125} It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 μM, respectively).{47058} Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide.{47059} Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels.{8975} It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ; Item No. 13104).{47060}
Brand:CaymanSKU:25503 - 25 gAvailable on backorder
Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels (IC50 = 184 nM for murine β-cells).{47058,34125} It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 μM, respectively).{47058} Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide.{47059} Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels.{8975} It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ; Item No. 13104).{47060}
Brand:CaymanSKU:25503 - 5 gAvailable on backorder
Glimepiride is a long-acting sulfonylurea that inhibits ATP-sensitive potassium (KATP) channels in pancreatic β-cells (IC50 = 3 nM), which leads to the release of insulin.{25521} At 20 μM, glimepiride has been shown to increase the activity of intracellular insulin receptors and to prevent insulin receptor downregulation during chronic insulin stimulation through a mechanism involving protein kinase C activation.{25523} It has been reported to be less effective at inhibiting nonpancreatic KATP channels, and therefore contributes fewer cardiac actions, compared to earlier generations of sulfonylurea anti-type 2 diabetes treatments.{25522}
Brand:CaymanSKU:12090 - 1 gAvailable on backorder
Glimepiride is a long-acting sulfonylurea that inhibits ATP-sensitive potassium (KATP) channels in pancreatic β-cells (IC50 = 3 nM), which leads to the release of insulin.{25521} At 20 μM, glimepiride has been shown to increase the activity of intracellular insulin receptors and to prevent insulin receptor downregulation during chronic insulin stimulation through a mechanism involving protein kinase C activation.{25523} It has been reported to be less effective at inhibiting nonpancreatic KATP channels, and therefore contributes fewer cardiac actions, compared to earlier generations of sulfonylurea anti-type 2 diabetes treatments.{25522}
Brand:CaymanSKU:12090 - 5 gAvailable on backorder
Glimepiride is a long-acting sulfonylurea that inhibits ATP-sensitive potassium (KATP) channels in pancreatic β-cells (IC50 = 3 nM), which leads to the release of insulin.{25521} At 20 μM, glimepiride has been shown to increase the activity of intracellular insulin receptors and to prevent insulin receptor downregulation during chronic insulin stimulation through a mechanism involving protein kinase C activation.{25523} It has been reported to be less effective at inhibiting nonpancreatic KATP channels, and therefore contributes fewer cardiac actions, compared to earlier generations of sulfonylurea anti-type 2 diabetes treatments.{25522}
Brand:CaymanSKU:12090 - 500 mgAvailable on backorder
Gliorosein is a fungal metabolite produced by Gliocladium.{38996} It is an isomer of rubrogliocladin hydroquinone. Gliorosein has antibiotic activity against B. allii, B. subtilis, and E. coli.
Brand:CaymanSKU:24921 - 1 mgAvailable on backorder
Gliorosein is a fungal metabolite produced by Gliocladium.{38996} It is an isomer of rubrogliocladin hydroquinone. Gliorosein has antibiotic activity against B. allii, B. subtilis, and E. coli.
Brand:CaymanSKU:24921 - 5 mgAvailable on backorder
Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi with diverse biological activities.{21692,21695,21694,21690,21693,21689,43859,21714} It inhibits 20S proteasomal chymotrypsin activity (IC50 = 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.{21695,21694} Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils.{21690,21693} It suppresses viral infection by Nipah and Hendra virus in HEK293T cells (IC50s = 149 and 579 nM, respectively).{21689} Under reducing conditions, gliotoxin inhibits leukotriene A4 hydrolase (LTA4H; Item No. 10007817) epoxide hydrolase activity, but not aminopeptidase activity, and leukotriene B4 (LTB4; Item No. 20110) synthesis in neutrophils and monocytes.{43859} In vivo, gliotoxin (5 mg/kg) reduces LTB4 plasma levels and blocks peritoneal neutrophil infiltration in a mouse model of peritonitis induced by zymosan A (Item No. 21175). It also inhibits geranylgeranyltransferase I and farnesyltransferase (IC50s = 17 and 80 μM, respectively).{21714}
Brand:CaymanSKU:11433 - 1 mgAvailable on backorder
Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi with diverse biological activities.{21692,21695,21694,21690,21693,21689,43859,21714} It inhibits 20S proteasomal chymotrypsin activity (IC50 = 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.{21695,21694} Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils.{21690,21693} It suppresses viral infection by Nipah and Hendra virus in HEK293T cells (IC50s = 149 and 579 nM, respectively).{21689} Under reducing conditions, gliotoxin inhibits leukotriene A4 hydrolase (LTA4H; Item No. 10007817) epoxide hydrolase activity, but not aminopeptidase activity, and leukotriene B4 (LTB4; Item No. 20110) synthesis in neutrophils and monocytes.{43859} In vivo, gliotoxin (5 mg/kg) reduces LTB4 plasma levels and blocks peritoneal neutrophil infiltration in a mouse model of peritonitis induced by zymosan A (Item No. 21175). It also inhibits geranylgeranyltransferase I and farnesyltransferase (IC50s = 17 and 80 μM, respectively).{21714}
Brand:CaymanSKU:11433 - 10 mgAvailable on backorder
Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi with diverse biological activities.{21692,21695,21694,21690,21693,21689,43859,21714} It inhibits 20S proteasomal chymotrypsin activity (IC50 = 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.{21695,21694} Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils.{21690,21693} It suppresses viral infection by Nipah and Hendra virus in HEK293T cells (IC50s = 149 and 579 nM, respectively).{21689} Under reducing conditions, gliotoxin inhibits leukotriene A4 hydrolase (LTA4H; Item No. 10007817) epoxide hydrolase activity, but not aminopeptidase activity, and leukotriene B4 (LTB4; Item No. 20110) synthesis in neutrophils and monocytes.{43859} In vivo, gliotoxin (5 mg/kg) reduces LTB4 plasma levels and blocks peritoneal neutrophil infiltration in a mouse model of peritonitis induced by zymosan A (Item No. 21175). It also inhibits geranylgeranyltransferase I and farnesyltransferase (IC50s = 17 and 80 μM, respectively).{21714}
Brand:CaymanSKU:11433 - 5 mgAvailable on backorder
Gliovirin is a fungal metabolite that has been found in T. harzianum and has fungicidal, antimicrobial and anti-inflammatory activities.{46408} It is active against the plant pathogenic fungus P. ultimum (MIC = 60 ng/ml) and the parasite T. brucei brucei (IC50 = 90 ng/ml), but has no effect on the plant pathogenic fungi R. solani, P. omnivorum, T. basicola, R. arrhizus, and V. dahliae or the bacteria B. thuringiensis, P. fluorescens, and X. malvacearum when used at concentrations up to 1,000 ng/ml.{46409,46410} Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50 = 1 µM) and protein levels of IL-2 in Jurkat cells (IC50 = 5.2 µM).{46408}
Brand:CaymanSKU:28583 - 1 mgAvailable on backorder
Glipizide is a hypoglycemic agent.{46791} It inhibits ATP-sensitive potassium (KATP) channels in primary mouse pancreatic β cells (IC50 = 6.4 nM). Glipizide induces insulin release from isolated rat pancreatic tissue with an EC50 value of 40 nM.{46792} Dietary administration of glipizide (5 mg/kg per day for 10 days) increases the number of insulin receptors on isolated and purified mouse liver plasma membranes.{46793} It reduces plasma glucose and triglyceride, but not total cholesterol, levels and increases plasma insulin levels in a rat model of diabetes induced by a high-fat diet and streptozotocin (STZ; Item No. 13104) when administered orally at a dose of 5 mg/kg.{46794} Formulations containing glipizide have been used in the treatment of type 2 diabetes.
Brand:CaymanSKU:11579 - 1 gAvailable on backorder
Glipizide is a hypoglycemic agent.{46791} It inhibits ATP-sensitive potassium (KATP) channels in primary mouse pancreatic β cells (IC50 = 6.4 nM). Glipizide induces insulin release from isolated rat pancreatic tissue with an EC50 value of 40 nM.{46792} Dietary administration of glipizide (5 mg/kg per day for 10 days) increases the number of insulin receptors on isolated and purified mouse liver plasma membranes.{46793} It reduces plasma glucose and triglyceride, but not total cholesterol, levels and increases plasma insulin levels in a rat model of diabetes induced by a high-fat diet and streptozotocin (STZ; Item No. 13104) when administered orally at a dose of 5 mg/kg.{46794} Formulations containing glipizide have been used in the treatment of type 2 diabetes.
Brand:CaymanSKU:11579 - 5 gAvailable on backorder
Glipizide-d11 is intended for use as an internal standard for the quantification of glipizide (Item No. 11579) by GC- or LC-MS. Glipizide is a hypoglycemic agent.{46791} It inhibits ATP-sensitive potassium (KATP) channels in primary mouse pancreatic β cells (IC50 = 6.4 nM). Glipizide induces insulin release from isolated rat pancreatic tissue with an EC50 value of 40 nM.{46792} Dietary administration of glipizide (5 mg/kg per day for 10 days) increases the number of insulin receptors on isolated and purified mouse liver plasma membranes.{46793} It reduces plasma glucose and triglyceride, but not total cholesterol, levels and increases plasma insulin levels in a rat model of diabetes induced by a high-fat diet and streptozotocin (STZ; Item No. 13104) when administered orally at a dose of 5 mg/kg.{46794} Formulations containing glipizide have been used in the treatment of type 2 diabetes.
Brand:CaymanSKU:30074 - 1 mgAvailable on backorder
Glipizide-d11 is intended for use as an internal standard for the quantification of glipizide (Item No. 11579) by GC- or LC-MS. Glipizide is a hypoglycemic agent.{46791} It inhibits ATP-sensitive potassium (KATP) channels in primary mouse pancreatic β cells (IC50 = 6.4 nM). Glipizide induces insulin release from isolated rat pancreatic tissue with an EC50 value of 40 nM.{46792} Dietary administration of glipizide (5 mg/kg per day for 10 days) increases the number of insulin receptors on isolated and purified mouse liver plasma membranes.{46793} It reduces plasma glucose and triglyceride, but not total cholesterol, levels and increases plasma insulin levels in a rat model of diabetes induced by a high-fat diet and streptozotocin (STZ; Item No. 13104) when administered orally at a dose of 5 mg/kg.{46794} Formulations containing glipizide have been used in the treatment of type 2 diabetes.
Brand:CaymanSKU:30074 - 500 µgAvailable on backorder
Gliquidone is a second generation sulfonylurea that selectively inhibits ATP-sensitive potassium channel currents (IKATP) in pancreatic β-cells (IC50s = 0.45, 119.1, and 149.7 µM for HIT-T15 cells, cardiomyocytes, and vascular smooth muscle cells, respectively).{49421} It is also a peroxisome proliferator-activated receptor γ (PPARγ) agonist (EC50 = 10 μM in a transactivation assay).{49422} Gliquidone (0.2 nmol/g) decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats.{49423} It decreases blood glucose levels, serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) activities, and hepatic lipid peroxidation and increases hepatic glutathione (GSH) levels in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 10 mg/kg.{49424}
Brand:CaymanSKU:29596 - 1 gAvailable on backorder
Gliquidone is a second generation sulfonylurea that selectively inhibits ATP-sensitive potassium channel currents (IKATP) in pancreatic β-cells (IC50s = 0.45, 119.1, and 149.7 µM for HIT-T15 cells, cardiomyocytes, and vascular smooth muscle cells, respectively).{49421} It is also a peroxisome proliferator-activated receptor γ (PPARγ) agonist (EC50 = 10 μM in a transactivation assay).{49422} Gliquidone (0.2 nmol/g) decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats.{49423} It decreases blood glucose levels, serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) activities, and hepatic lipid peroxidation and increases hepatic glutathione (GSH) levels in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 10 mg/kg.{49424}
Brand:CaymanSKU:29596 - 10 gAvailable on backorder
Gliquidone is a second generation sulfonylurea that selectively inhibits ATP-sensitive potassium channel currents (IKATP) in pancreatic β-cells (IC50s = 0.45, 119.1, and 149.7 µM for HIT-T15 cells, cardiomyocytes, and vascular smooth muscle cells, respectively).{49421} It is also a peroxisome proliferator-activated receptor γ (PPARγ) agonist (EC50 = 10 μM in a transactivation assay).{49422} Gliquidone (0.2 nmol/g) decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats.{49423} It decreases blood glucose levels, serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) activities, and hepatic lipid peroxidation and increases hepatic glutathione (GSH) levels in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 10 mg/kg.{49424}
Brand:CaymanSKU:29596 - 5 gAvailable on backorder
Gliquidone is a second generation sulfonylurea that selectively inhibits ATP-sensitive potassium channel currents (IKATP) in pancreatic β-cells (IC50s = 0.45, 119.1, and 149.7 µM for HIT-T15 cells, cardiomyocytes, and vascular smooth muscle cells, respectively).{49421} It is also a peroxisome proliferator-activated receptor γ (PPARγ) agonist (EC50 = 10 μM in a transactivation assay).{49422} Gliquidone (0.2 nmol/g) decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats.{49423} It decreases blood glucose levels, serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) activities, and hepatic lipid peroxidation and increases hepatic glutathione (GSH) levels in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 10 mg/kg.{49424}
Brand:CaymanSKU:29596 - 500 mgAvailable on backorder
Globosuxanthone A is a fungal metabolite originally isolated from C. globosum.{48211} It is cytotoxic to various human solid tumor cell lines, including MCF-7, PC3, LNCap, and DU145 cells (IC50s = 1.3, 0.65, 1.5, and 1.2 µM, respectively). It induces accumulation of cells in the G2/M and S phases of the cell cycle in NCI-H460 and PC3M cells. Globosuxanthone A is also active against C. albicans but not S. aureus, E. coli, or M. hiemalis.{48212}
Brand:CaymanSKU:27486 - 1 mgAvailable on backorder
Globosuxanthone A is a fungal metabolite originally isolated from C. globosum.{48211} It is cytotoxic to various human solid tumor cell lines, including MCF-7, PC3, LNCap, and DU145 cells (IC50s = 1.3, 0.65, 1.5, and 1.2 µM, respectively). It induces accumulation of cells in the G2/M and S phases of the cell cycle in NCI-H460 and PC3M cells. Globosuxanthone A is also active against C. albicans but not S. aureus, E. coli, or M. hiemalis.{48212}
Brand:CaymanSKU:27486 - 5 mgAvailable on backorder
Globosuxanthone A is a fungal metabolite originally isolated from C. globosum.{48211} It is cytotoxic to various human solid tumor cell lines, including MCF-7, PC3, LNCap, and DU145 cells (IC50s = 1.3, 0.65, 1.5, and 1.2 µM, respectively). It induces accumulation of cells in the G2/M and S phases of the cell cycle in NCI-H460 and PC3M cells. Globosuxanthone A is also active against C. albicans but not S. aureus, E. coli, or M. hiemalis.{48212}
Brand:CaymanSKU:27486 - 500 µgAvailable on backorder
Globotetraosylceramides are bioactive neutral glycosphingolipids. They are the major glycolipids in human erythrocytes.{43016} They act as receptors for the Shiga toxins Stx1, Stx2, and Stx2e, the cytotoxic protein pierisin-1, and parvovirus B19.{43017,43018,43019} Globotetraosylceramides increase the expression of proteins responsible for enamel deposition, including ameloblastin, amelogenin, and enamelin, in dental epithelial cells and activate the ERK and p38 MAPK signaling pathways.{43020} Levels of globotetraosylceramides are elevated in fibroblasts from patients with salt and pepper syndrome, a neurocutaneous condition characterized by intellectual disability and hyper- and hypo-pigmented skin.{43021} Globotetraosylceramides (porcine RBC) contains a mixture of globotetraosylceramides with variable fatty acyl chain lengths isolated from porcine red blood cells. [Matreya, LLC. Catalog No. 1068]
Brand:CaymanSKU:24881 - 5 mgAvailable on backorder
Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides (Item No. 16983).{38975} They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo.{38976} Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A.{38977} Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes.{38975} This product contains a mixture of hydroxy and non-hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs). [Matreya, LLC. Catalog No. 1067]
Brand:CaymanSKU:24870 - 1 mgAvailable on backorder
Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides (Item No. 16983).{38975} They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo.{38976} Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A.{38977} Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes.{38975} This product contains a mixture of hydroxy and non-hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs). [Matreya, LLC. Catalog No. 1067]
Brand:CaymanSKU:24870 - 10 mgAvailable on backorder
GLP-1R agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).{46660} It inhibits forskolin-induced cAMP accumulation in BHK cells expressing the recombinant human receptor with an EC50 value of 101 nM.{46661} GLP-1R (100 and 1,000 nM) increases insulin levels induced by D-(+)-glucose (Item No. 23733) in pancreatic islets isolated from wild-type, but not Glp1r knockout, mice. It reduces fasting plasma glucose levels in mice when administered at a dose of 5 µmol/kg.{46662}
Brand:CaymanSKU:29678 - 1 mgAvailable on backorder
GLP-1R agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).{46660} It inhibits forskolin-induced cAMP accumulation in BHK cells expressing the recombinant human receptor with an EC50 value of 101 nM.{46661} GLP-1R (100 and 1,000 nM) increases insulin levels induced by D-(+)-glucose (Item No. 23733) in pancreatic islets isolated from wild-type, but not Glp1r knockout, mice. It reduces fasting plasma glucose levels in mice when administered at a dose of 5 µmol/kg.{46662}
Brand:CaymanSKU:29678 - 10 mgAvailable on backorder
GLP-1R agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).{46660} It inhibits forskolin-induced cAMP accumulation in BHK cells expressing the recombinant human receptor with an EC50 value of 101 nM.{46661} GLP-1R (100 and 1,000 nM) increases insulin levels induced by D-(+)-glucose (Item No. 23733) in pancreatic islets isolated from wild-type, but not Glp1r knockout, mice. It reduces fasting plasma glucose levels in mice when administered at a dose of 5 µmol/kg.{46662}
Brand:CaymanSKU:29678 - 25 mgAvailable on backorder
GLP-1R agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).{46660} It inhibits forskolin-induced cAMP accumulation in BHK cells expressing the recombinant human receptor with an EC50 value of 101 nM.{46661} GLP-1R (100 and 1,000 nM) increases insulin levels induced by D-(+)-glucose (Item No. 23733) in pancreatic islets isolated from wild-type, but not Glp1r knockout, mice. It reduces fasting plasma glucose levels in mice when administered at a dose of 5 µmol/kg.{46662}
Brand:CaymanSKU:29678 - 5 mgAvailable on backorder
GLPG0187 is a nonpeptide antagonist of αν integrin receptors (IC50s = 1.2-3.7 nM).{38088} It inhibits osteoclastogenesis, bone resorption, and angiogenesis in vitro and in vivo in mice, which are all hallmarks of bone marrow invasion in metastatic prostate cancer. GLPG0187 reduces epithelial-mesenchymal transition (EMT) and migration of PC-3M-Pro4/luc cells in a dose-dependent manner without inhibiting cell growth. GLPG0187 also induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells.{38089} Formulations containing GLPG0187 are being tested in Phase I clinical trials for the treatment of high-grade gliomas and other advanced solid malignancies.{38090}
Brand:CaymanSKU:21792 -Out of stock
GLPG0187 is a nonpeptide antagonist of αν integrin receptors (IC50s = 1.2-3.7 nM).{38088} It inhibits osteoclastogenesis, bone resorption, and angiogenesis in vitro and in vivo in mice, which are all hallmarks of bone marrow invasion in metastatic prostate cancer. GLPG0187 reduces epithelial-mesenchymal transition (EMT) and migration of PC-3M-Pro4/luc cells in a dose-dependent manner without inhibiting cell growth. GLPG0187 also induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells.{38089} Formulations containing GLPG0187 are being tested in Phase I clinical trials for the treatment of high-grade gliomas and other advanced solid malignancies.{38090}
Brand:CaymanSKU:21792 -Out of stock
GLPG0187 is a nonpeptide antagonist of αν integrin receptors (IC50s = 1.2-3.7 nM).{38088} It inhibits osteoclastogenesis, bone resorption, and angiogenesis in vitro and in vivo in mice, which are all hallmarks of bone marrow invasion in metastatic prostate cancer. GLPG0187 reduces epithelial-mesenchymal transition (EMT) and migration of PC-3M-Pro4/luc cells in a dose-dependent manner without inhibiting cell growth. GLPG0187 also induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells.{38089} Formulations containing GLPG0187 are being tested in Phase I clinical trials for the treatment of high-grade gliomas and other advanced solid malignancies.{38090}
Brand:CaymanSKU:21792 -Out of stock
GLPG0492 is a selective androgen receptor modulator (SARM).{53473} It activates the androgen receptor in a transactivation assay (EC50 = 12 nM in HeLa cells expressing the human receptor). GLPG0492 (10 mg/kg per day) increases levator ani muscle weight, a marker of anabolic activity, but has no effect on ventral prostate weight, a marker of androgenic activity, in castrated rats. It increases twitch tension in isolated diaphragm strips, as well as increases the total distance run in a treadmill test and decreases gastrocnemius muscle fibrosis in the exercised-mdx mouse model of muscular dystrophy when administered at a dose of 30 mg/kg.{53474} GLPG0492 also reverses immobilization-induced muscle atrophy in a mouse model of hindlimb immobilization.{53475}
Brand:CaymanSKU:29938 - 1 mgAvailable on backorder
GLPG0974 is an antagonist of free fatty acid receptor 2 (FFAR2/GPR43; IC50 = 9 nM).{46506} It is selective for FFAR2 over FFAR3 at concentrations up to 30 μM and over a panel of 55 receptors, ion channels, and transporters at 10 μM. GLPG0974 inhibits acetate-induced migration of isolated human neutrophils in buffer or plasma (IC50s = 27 and 43 nM, respectively), as well as acetate-induced expression of CD11b activation-specific epitope on neutrophils in isolated human whole blood (IC50 = 438 nM). GLPG0974 also inhibits a human FFAR2-based designer receptor exclusively activated by designer drugs (hFFAR2-DREADD; IC50 = 36.31 nM in a cell-based β-arrestin-2 recruitment assay).{46507} It inhibits glucagon-like peptide 1 (GLP-1) secretion induced by the hFFA2-DREADD ligand sorbic acid in isolated colonic crypts from mice expressing hemagglutinin-tagged hFFAR2-DREADD when used at a concentration of 10 μM.
Brand:CaymanSKU:28108 - 1 mgAvailable on backorder
GLPG0974 is an antagonist of free fatty acid receptor 2 (FFAR2/GPR43; IC50 = 9 nM).{46506} It is selective for FFAR2 over FFAR3 at concentrations up to 30 μM and over a panel of 55 receptors, ion channels, and transporters at 10 μM. GLPG0974 inhibits acetate-induced migration of isolated human neutrophils in buffer or plasma (IC50s = 27 and 43 nM, respectively), as well as acetate-induced expression of CD11b activation-specific epitope on neutrophils in isolated human whole blood (IC50 = 438 nM). GLPG0974 also inhibits a human FFAR2-based designer receptor exclusively activated by designer drugs (hFFAR2-DREADD; IC50 = 36.31 nM in a cell-based β-arrestin-2 recruitment assay).{46507} It inhibits glucagon-like peptide 1 (GLP-1) secretion induced by the hFFA2-DREADD ligand sorbic acid in isolated colonic crypts from mice expressing hemagglutinin-tagged hFFAR2-DREADD when used at a concentration of 10 μM.
Brand:CaymanSKU:28108 - 5 mgAvailable on backorder
GLP1690 is a potent inhibitor of autotaxin (Ki = 15 nM).{36941} It inhibits the production of lysophosphatidic acid (LPA) in mouse, rat, and human plasma (IC50s = 418, 542, and 242 nM, respectively). GLPG1690 (30 mg/kg) reduces extracellular matrix deposition in the lung as well as LPA 18:2 levels in bronchoalveolar lavage fluid in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877).
Brand:CaymanSKU:25498 - 10 mgAvailable on backorder
GLP1690 is a potent inhibitor of autotaxin (Ki = 15 nM).{36941} It inhibits the production of lysophosphatidic acid (LPA) in mouse, rat, and human plasma (IC50s = 418, 542, and 242 nM, respectively). GLPG1690 (30 mg/kg) reduces extracellular matrix deposition in the lung as well as LPA 18:2 levels in bronchoalveolar lavage fluid in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877).
Brand:CaymanSKU:25498 - 25 mgAvailable on backorder
GLP1690 is a potent inhibitor of autotaxin (Ki = 15 nM).{36941} It inhibits the production of lysophosphatidic acid (LPA) in mouse, rat, and human plasma (IC50s = 418, 542, and 242 nM, respectively). GLPG1690 (30 mg/kg) reduces extracellular matrix deposition in the lung as well as LPA 18:2 levels in bronchoalveolar lavage fluid in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877).
Brand:CaymanSKU:25498 - 5 mgAvailable on backorder
GLP1690 is a potent inhibitor of autotaxin (Ki = 15 nM).{36941} It inhibits the production of lysophosphatidic acid (LPA) in mouse, rat, and human plasma (IC50s = 418, 542, and 242 nM, respectively). GLPG1690 (30 mg/kg) reduces extracellular matrix deposition in the lung as well as LPA 18:2 levels in bronchoalveolar lavage fluid in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877).
Brand:CaymanSKU:25498 - 50 mgAvailable on backorder
GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR).{52061,52059} It increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508 deletion (F508del) and G551D missense mutations with EC50 values of 88, 3, and 339 nM, respectively, in a reporter assay. GLPG1837 increases forskolin-induced conductivity of patient-derived bronchial epithelial cells expressing both F508del- and G551D-mutant CFTRs (EC50 = 159 nM in a transepithelial clamp circuit (TECC) assay).{52061}
Brand:CaymanSKU:9003143 - 1 mgAvailable on backorder
GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR).{52061,52059} It increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508 deletion (F508del) and G551D missense mutations with EC50 values of 88, 3, and 339 nM, respectively, in a reporter assay. GLPG1837 increases forskolin-induced conductivity of patient-derived bronchial epithelial cells expressing both F508del- and G551D-mutant CFTRs (EC50 = 159 nM in a transepithelial clamp circuit (TECC) assay).{52061}
Brand:CaymanSKU:9003143 - 10 mgAvailable on backorder
GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR).{52061,52059} It increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508 deletion (F508del) and G551D missense mutations with EC50 values of 88, 3, and 339 nM, respectively, in a reporter assay. GLPG1837 increases forskolin-induced conductivity of patient-derived bronchial epithelial cells expressing both F508del- and G551D-mutant CFTRs (EC50 = 159 nM in a transepithelial clamp circuit (TECC) assay).{52061}
Brand:CaymanSKU:9003143 - 25 mgAvailable on backorder
GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR).{52061,52059} It increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508 deletion (F508del) and G551D missense mutations with EC50 values of 88, 3, and 339 nM, respectively, in a reporter assay. GLPG1837 increases forskolin-induced conductivity of patient-derived bronchial epithelial cells expressing both F508del- and G551D-mutant CFTRs (EC50 = 159 nM in a transepithelial clamp circuit (TECC) assay).{52061}
Brand:CaymanSKU:9003143 - 5 mgAvailable on backorder
GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50 = 0.021 μM).{50176} It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cells in vitro (GI50 = 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model.
Brand:CaymanSKU:28581 - 1 mgAvailable on backorder
GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50 = 0.021 μM).{50176} It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cells in vitro (GI50 = 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model.
Brand:CaymanSKU:28581 - 10 mgAvailable on backorder
GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50 = 0.021 μM).{50176} It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cells in vitro (GI50 = 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model.
Brand:CaymanSKU:28581 - 5 mgAvailable on backorder