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ND-630

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产品信息

产品名称：ND-630	纯度：98%min
CAS NO：1434635-54-7	溶解度：Soluble in DMSO
分子式：C₂₈H₃₁N₃O₈S	包装：可按客户要求包装。
分子量：569.63	贮存：Store at -20℃ 3 years

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备注说明

ND-630 is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC₅₀ values of 2.1 and 6.1 nM, respectively.ND-630 inhibits hACC1 (IC₅₀=2.1±0.2 nM) and hACC2 (IC₅₀=6.1±0.8 nM). Inhibition is reversible and highly specific for ACC. ND-630 inhibits ACC activity by interacting within the phosphopeptide-acceptor and dimerization site of the enzyme to prevent dimerization. ND-630 inhibits fatty acid synthesis with an EC₅₀ of 66 nM in HepG2 cells without altering the total cell number, cellular protein concentration, and incorporation of acetate into cholesterol^[1].Chronical administration of 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 ND-630 Zucker diabetic fatty rats, ND-630 reduces hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction). ND-630 exhibits an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. Pharmacokinetic evaluation of ND-630 in male Sprague–Dawley rats [i.v. 3 mg/kg; orally (p.o.) 10 mg/kg] yields a plasma t_1/2 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].

参考文献

[1]. Harriman G, 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 Mar 29;113(13):E1796-805.