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CAS No.: 1434635-54-7

Firsocostat Catalog No. CSN21232

Synonyms: ND-630;GS-0976;NDI-010976

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).

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技术信息

生物活性

描述Fatty acid metabolism dysregulated through elevated fatty acid synthesis (FASyn), impaired fatty acid oxidation (FAOxn), or both is a hallmark of various metabolic disorders. ACC (acetyl-CoA carboxylase) catalyzes the ATP-dependent carboxylation of acetyl-CoA to form malonyl-CoA, the rate-limiting and first committed reaction in FASyn. ND-630, a reversible and highly specific ACC inhibitor, inhibits hACC1 with an IC₅₀ of 2.1 ± 0.2 nM and hACC2 with an IC₅₀ of 6.1 ± 0.8 nM. When ND-630 and [¹⁴C]acetate were administered to Hep-G2 cells for 4 h, ND-630 inhibited FASyn with EC₅₀ values of 66 nM in cells cultured in medium containing 10% serum and 8.7 nM when assessed in serum-free medium. When ND-630 and [¹⁴C]palmitate were administered to C2C12 cells for 6 h, ND-630 increased both the release of [¹⁴C]O₂ and the production of [¹⁴C]acid-soluble material. ND-630 exhibited an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. When chow-fed male Sprague–Dawley rats were treated orally with ND-630 for 1 h, hepatic malonyl-CoA was dose-dependently reduced with an ED₅₀ of 0.8 mg/kg. When chow-fed male Sprague–Dawley rats treated orally with ND-630 for 1 h were given an i.p. bolus of [¹⁴C]acetate, ND-630 reduced hepatic FASyn with an ED₅₀ of 0.14 mg/kg. Moreover, ND-630 increased whole-body FAOxn, assessed as a reduction in respiratory quotient (RQ). As a consequence of FASyn inhibition and FAOxn stimulation, ND-630 dose-dependently reduced the hepatic steatosis produced by the HSD (high-sucrose diet) without altering either hepatic cholesterol or glycogen. ND-630 also dose-dependently reduced the elevated plasma triglycerides and free fatty acids produced by the HSD^[1].
作用机制ND-630 interacts within the acetyl-CoA carboxylase subunit phosphopeptide acceptor and dimerization site to prevent dimerization and inhibit enzymatic activity^[1].
参考文献

[1] Harriman G, Greenwood J, Bhat S, et al. Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats. Proc Natl Acad Sci U S A. 2016;113(13):E1796-E1805.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7555 mL
- 8.7776 mL
- 17.5553 mL
- 5 mM
- 0.3511 mL
- 1.7555 mL
- 3.5111 mL
- 10 mM
- 0.1756 mL
- 0.8778 mL
- 1.7555 mL

技术信息

CAS号

1434635-54-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H31N3O8S

运输

蓝冰

分子量

569.63

别名

ND-630;GS-0976;NDI-010976;ND630. NDI-010976;firsocostat

溶解度

DMSO	215.0 mg/mL (377.4 mM)
Water	insoluble

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