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 国际站：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：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Anti-diabetic Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Anti-Obesity Compound Library  |  Lipid Metabolism Compound Library   |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  hACC2-IN-1  |  Moiramide B  |  ND-646  |  Sethoxydim  |  Firsocostat (S enantiomer)  |  CP-640186 hydrochloride  |  CP-610431  |  ACC1/2-IN-2  |  MK-4074  |  Acetyl-CoA Carboxylase-IN-1  |  CMS-121  |  PF-05175157  |  S-2E  |  Fluazifop-P-butyl  |  A-908292  |  Haloxyfop  |  TOFA  |  ACC1/2-IN-1  |  Olumacostat glasaretil  |  Propaquizafop

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 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；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。