化合物ND-630 T7184

Product Introduction
Bioactivity


英文名: Firsocostat

描述: Firsocostat (GS-0976) 是有效的乙酰辅酶A 羧化酶 (ACC) 抑制剂，抑制人类 ACC1 和 ACC2 的IC50分别为2.1和6.1 nM。

体外活性: ND-630 inhibited hACC1 with an IC50 of 2.1 ± 0.2 nM and hACC2 with an IC50 of 6.1 ± 0.8 nM .?Inhibition was reversible and highly specific for ACC, as evidenced by the absence of an effect of ND-630 on the activity of 101 enzymes, receptors, growth factors, transporters, and ion channels of the Ricerca DrugMatrix Panel at 10 μM .?In addition, because the ACC dimerization site is not conserved among the mammalian carboxylases , ND-630 lacks the ability to inhibit any of these mechanistically related enzymes and therefore exhibits absolute specificity for ACC inhibition relative to other mammalian carboxylases.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (105.33 mM)


关键字: NDI 010976 | Acetyl-CoA Carboxylase | ND 630 | Firsocostat | GS0976 | inhibit | NDI010976 | ACC, Acetyl Coenzyme A Carboxylase | Inhibitor | GS 0976 | ND630

相关产品: PF-05221304 | ND-646 | PF-05175157 | CP-640186 hydrochloride | Haloxyfop | Olumacostat Glasaretil | Moiramide B | TOFA | Tralkoxydim | CP-640186

相关库: Drug Repurposing Compound Library | Anti-Hypertension Compound Library | ReFRAME Related Library | Clinical Compound Library | Human Metabolite Library | Inhibitor Library | Metabolism Compound Library | Target-Focused Phenotypic Screening Library | Preclinical Compound Library | Anti-Cardiovascular Disease Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途