Identification | Back Directory | [Name]
NDI-010976 | [CAS]
1434635-54-7 | [Synonyms]
ND-630 GS0976 CS-2609 CS-2632 CPDB5078 EOS-61252 NDI-010976 Firsocostat GS0976,ND-630 ND-630,NDI-010976 ND630;FIRSOCOSTAT Firsocostat (ND-630 Firsocostat(ND-630,GS-0976) Firsocostat (GS-0976,NDI-010976,ND-630) ND 630; ND630;GS-0976;GS 0976;GS0976;FIRSOCOSTAT (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- 1,4-Dihydro-1-[(2R)-2-(2-methoxyphenyl)-2-[(tetrahydro-2H-pyran-4-yl)oxy]ethyl]-α,α,5-trimethyl-6-(2-oxazolyl)-2,4-dioxothieno[2,3-d]pyrimidine-3(2H)-acetic acid Thieno[2,3-d]pyrimidine-3(2H)-acetic acid, 1,4-dihydro-1-[(2R)-2-(2-methoxyphenyl)-2-[(tetrahydro-2H-pyran-4-yl)oxy]ethyl]-α,α,5-trimethyl-6-(2-oxazolyl)-2,4-dioxo- (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 (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 | [Molecular Formula]
C28H31N3O8S | [MDL Number]
MFCD28963986 | [MOL File]
1434635-54-7.mol | [Molecular Weight]
569.63 |
Chemical Properties | Back Directory | [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 |
Hazard Information | Back Directory | [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).1 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. |
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