Firsocostat | Allosteric acetyl-CoA carboxylase inhibitor

CAS:
1434635-54-7
Catalog Number:
10-4699
Activity:
Allosteric ACC inhibitor
Chemical Names:
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
Alternate Name:
ND-630; NDI-010976; GS-0976
Molecular Weight:
569.63
Molecular Formula:
C28H31N3O8S
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
white solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$75.00
25 mg$235.00
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Firsocostat (1434635-54-7) is a 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

References/Citations:

  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
CAS:
1434635-54-7
Catalog Number:
10-4699
Activity:
Allosteric ACC inhibitor
Chemical Names:
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
Alternate Name:
ND-630; NDI-010976; GS-0976
Molecular Weight:
569.63
Molecular Formula:
C28H31N3O8S
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
white solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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