NDI-010976
NDI-010976 Basic information
- Product Name:
- NDI-010976
- Synonyms:
-
- NDI-010976
- (R)-2-(1-(2-(2-methoxyphenyl)-2-((tetrahydro-2H-pyran-4-yl)oxy)ethyl)-5-methyl-6-(oxazol-2-yl)-2,4-dioxo-1,4-dihydrothieno[2,3-d]pyrimidin-3(2H)-yl)-2-methylpropanoicacid
- ND-630
- (R)-2-(1-(2-(2-methoxyphenyl)-2-((tetrahydro-2H-pyran-4-yl)oxy)ethyl)-5-methyl-6-(oxazol-2-yl)-2,4-dioxo-1,2-dihydrothieno[2,3-d]pyrimidin-3(4H)-yl)-2-methylpropanoic acid
- EOS-61252
- GS0976
- CPDB5078
- (R)-2-(1-(2-(2-methoxyphenyl)-2-((tetrahydro-2H-pyran-4-yl)oxy)ethyl)-5-methyl-6-(oxazol-2-yl)-2,4-dioxo-1,2-dihydrothieno[2,3-
- CAS:
- 1434635-54-7
- MF:
- C28H31N3O8S
- MW:
- 569.63
- Product Categories:
-
- API
- Mol File:
- 1434635-54-7.mol
NDI-010976 Chemical Properties
- Boiling point:
- 779.0±70.0 °C(Predicted)
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:75.0(Max Conc. mg/mL);131.66(Max Conc. mM)
DMF:10.0(Max Conc. mg/mL);17.56(Max Conc. mM)
Ethanol:3.0(Max Conc. mg/mL);5.27(Max Conc. mM) - form
- A crystalline solid
- pka
- 3.66±0.10(Predicted)
- color
- White to light yellow
- InChIKey
- ZZWWXIBKLBMSCS-XKGZFIRZNA-N
- SMILES
- C(O)(=O)C(N1C(=O)N(C[C@@H](C2=CC=CC=C2OC)OC2CCOCC2)C2SC(C3=NC=CO3)=C(C)C=2C1=O)(C)C |&1:9,r|
NDI-010976 Usage And Synthesis
Description
ND-630 is an allosteric inhibitor of acetyl-CoA carboxylase (ACC) dimerization that inhibits ACC1 and ACC2 activity (IC50s = 2.1 and 6.1 nM, respectively, for the human enzymes). It is selective for ACC over 101 enzymes, receptors, growth factors, transporters, and ion channels up to a concentration of 10 μM. ND-630 prevents dimerization of ACC by interacting within the phosphopeptide-acceptor and dimerization site. It reduces fatty acid synthesis (EC50s = 66 and 9 nM in 10% FBS and serum-free media, respectively) and increases fatty acid oxidation in HepG2 cells. ND-630 reduces hepatic steatosis in a rat model of diet-induced obesity and in Zucker diabetic rats. It also improves insulin secretion stimulated by glucose and reduces hemoglobin A1c levels by 0.9% in Zucker diabetic rats.
Uses
Firsocostat or ND-630 (CAS# 1434635-54-7) is an inhibitor of acetyl-coA carboxylase and may favorably affect the morbidity and mortality associated with obesity, diabetes, and fatty liver disease from reduced hepatic steatosis, improved insulin sensitivity, and modulation of dyslipidemia.
in vivo
Chronical administration of Firsocostat (ND-630) to rats with diet-induced obesity reduces hepatic steatosis, improves insulin sensitivity, reduces weight gain without affecting food intake, and favorably affects dyslipidemia. Chronical administration of Firsocostat Zucker diabetic fatty rats, Firsocostat reduces hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction). Firsocostat exhibits an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. Pharmacokinetic evaluation of Firsocostat in male Sprague-Dawley rats [i.v. 3 mg/kg; orally (p.o.) 10 mg/kg] yields a plasma t1/2 of 4.5 h, bioavailability of 37%, clearance of 33 mL/min/kg, volume of distribution of 1.9 L/kg, oral time of maximum plasma concentration of 0.25 h[1].
References
[1] G. HARRIMAN. Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats[J]. Proceedings of the National Academy of Sciences, 2016, 43 1: E1796-E1805. DOI: 10.1073/pnas.1520686113
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