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Supplier 1434635-54-7 on hot selling NDI-010976 Manufacturer CAS NO.1434635-54-7
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Superiority
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.
ND-630, also known as GS-0976, NDI-010976, and firsocostat, is a potent ACC inhibitor. ND-630 nteracts within the ACC phosphopeptide acceptor and dimerization site to prevent dimerization and inhibit the enzymatic activity of both ACC iso-zymes, reduce fatty acid synthesis and stimulate fatty acid oxidation in cultured cells and in animals, and exhibit favorable drug-like properties. ND-630 reduces hepatic steatosis, improves insulin sensitivity, reduces weight gain without affecting food intake, and favorably affects dyslipidemia. When administered chronically to Zucker diabetic fatty rats, ND-630 reduces
hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction).
hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction).
Details
ND-630, also called as NDI 010976, is a highly selective, reversible inhibitor of acetyl-CoA carboxylase (ACC) and had IC50 values of 2 and 7 nM for ACC1 and 2, respectively, EC50 values in HepG2 serum free and 10% serum of 9 and 66 nM, respectively, and 2-fold C2C12 fatty acid oxidation (FAOxn) stimulation at 200 nM.
| Name | ND-630 |
|---|---|
| Iupac Chemical Name | 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-thieno[2,3-d]pyrimidine-3(2H)-acetic acid |
| Synonyms | ND-630; ND 630; ND630. NDI-010976; NDI 010976; NDI010976; GS-0976; GS0976; GS 0976; firsocostat; |
| Molecular Formula | C28H31N3O8S |
| Molecular Weight | 569.629 |
| Smile | O=C(O)C(C)(C)N(C(N(C[C@@H](C1=CC=CC=C1OC)OC2CCOCC2)C3=C4C(C)=C(C5=NC=CO5)S3)=O)C4=O |
| InChiKey | ZZWWXIBKLBMSCS-FQEVSTJZSA-N |
| InChi | InChI=1S/C28H31N3O8S/c1-16-21-24(32)31(28(2,3)26(33)34)27(35)30(25(21)40-22(16)23-29-11-14-38-23)15-20(39-17-9-12-37-13-10-17)18-7-5-6-8-19(18)36-4/h5-8,11,14,17,20H,9-10,12-13,15H2,1-4H3,(H,33,34)/t20-/m0/s1 |
| CAS Number | 1434635-54-7 |