MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Firsocostat

CAS No. : 1434635-54-7

MCE 站：Firsocostat

产品活性：Firsocostat (ND-630; GS-0976; NDI-010976) 是乙酰辅酶A羧化酶 (ACC) 抑制剂，抑制人类 ACC1 和 ACC2 的 IC₅₀ 值分别为2.1和6.1 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acetyl-CoA Carboxylase

In Vitro: Firsocostat (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. Firsocostat inhibits ACC activity by interacting within the phosphopeptide-acceptor and dimerization site of the enzyme to prevent dimerization. Firsocostat 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.

In Vivo: Chronical administration of Firsocostat (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 Firsocostat Zucker diabetic fatty rats, Firsocostat reduces hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction). Firsocostat exhibits an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. Pharmacokinetic evaluation of Firsocostat 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Diabetes Related Compound Library  |  TOFA  |  Fluazifop-P-butyl  |  Propaquizafop

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。