Firsocostat
Firsocostat
Firsocostat
| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-4699-5MG | Firsocostat | 5mg | $158.00 | |
| GBM-4699-25MG | Firsocostat | 25mg | $494.00 |
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Description
Allosteric acetyl-CoA carboxylase inhibitor
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Specifications
Bioassays Specification Bio-Activity Allosteric acetyl-CoA carboxylase inhibitor Chemical Name 2-[1-[(2R)-2-(2-Methoxyphenyl)-2-9oxan-4-yloxy)ethyl]-5-methyl-6-(1,3-oxazol-2-yl)-2,4-dioxothieno[2,3-d]pyrimidin-3-yl]-2-methylpropanoic acid Function / Pharmacology Potent (IC50 = 1.7 nM ACC1; 2.6 nM ACC2) allosteric protein-protein interaction inhibitor of acetyl-CoA carboxylase (ACC).1 It interacts with the ACC phosphopeptide acceptor and dimerization site to inhibit enzymatic activity resulting in decreased fatty acid synthesis and stimulation of fatty acid oxidation. It reduced hepatic steatosis, improves insulin sensitivity, reduces weight gain, and favorably affects dyslipidemia in rats. Firsocostat decreased hepatic steatosis and fibrosis markers in patients with nonalcoholic fatty liver disease.2 Directly impairs profibrinogenic activity of hepatic stellate cells (HSC) via prevention of induction of glycolysis and oxidative phosphorylation during HSC activation.3 CAS# 1434635-54-7 MW 569.63 Molecular Formula C28H31N3O8S Solubility Soluble in DMSO (up to at least 25 mg/ml) Supplied powder Storage as supplied -20°C Ship temp Ambient References 1) Harriman et al. (2016), Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats; Proc. Nat. Acad. Sci. USA, 113 E1796 2) Looma et al. (2018), GS-0976 Reduces Hepatic Steatosis and Fibrosis Markers in Patients With Nonalcoholic Fatty Liver Disease; Gastroenterology, 155 1463 3) Bates et al. (2020), Acetyl-CoA carboxylase inhibition disrupts metabolic reprogramming during hepatic stellate cell activation; J. Hepatol., 73 896 Antibody Specification Alternate Names ND-630; NDI-010976; GS-0976 Protein Specification Purity >98% - Reviews
| Bioassays Specification | |
| Bio-Activity | Allosteric acetyl-CoA carboxylase inhibitor |
| Chemical Name | 2-[1-[(2R)-2-(2-Methoxyphenyl)-2-9oxan-4-yloxy)ethyl]-5-methyl-6-(1,3-oxazol-2-yl)-2,4-dioxothieno[2,3-d]pyrimidin-3-yl]-2-methylpropanoic acid |
| Function / Pharmacology | Potent (IC50 = 1.7 nM ACC1; 2.6 nM ACC2) allosteric protein-protein interaction inhibitor of acetyl-CoA carboxylase (ACC).1 It interacts with the ACC phosphopeptide acceptor and dimerization site to inhibit enzymatic activity resulting in decreased fatty acid synthesis and stimulation of fatty acid oxidation. It reduced hepatic steatosis, improves insulin sensitivity, reduces weight gain, and favorably affects dyslipidemia in rats. Firsocostat decreased hepatic steatosis and fibrosis markers in patients with nonalcoholic fatty liver disease.2 Directly impairs profibrinogenic activity of hepatic stellate cells (HSC) via prevention of induction of glycolysis and oxidative phosphorylation during HSC activation.3 |
| CAS# | 1434635-54-7 |
| MW | 569.63 |
| Molecular Formula | C28H31N3O8S |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 1) Harriman et al. (2016), Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats; Proc. Nat. Acad. Sci. USA, 113 E1796 2) Looma et al. (2018), GS-0976 Reduces Hepatic Steatosis and Fibrosis Markers in Patients With Nonalcoholic Fatty Liver Disease; Gastroenterology, 155 1463 3) Bates et al. (2020), Acetyl-CoA carboxylase inhibition disrupts metabolic reprogramming during hepatic stellate cell activation; J. Hepatol., 73 896 |
| Antibody Specification | |
| Alternate Names | ND-630; NDI-010976; GS-0976 |
| Protein Specification | |
| Purity | >98% |