产品名称

PF-05175157

一般描述

PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively.

别称

1,4-Dihydro-1′-[(2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-spiro[5H indazole-5,4′-piperidin]-7(6H)-one, 1-Isopropyl-1-(2-methyl-1H-benzo[d]imidazole-6-carbonyl)-1,4-dihydrospiro[indazole-5,4-piperidin]-7(6H)-one

纯 度

≥98.0%(HPLC)

CAS NO.

1301214-47-0

分子式

C²³H²⁷N⁵O²

分子量

405.49

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至米色固体

溶解性(25℃)

DMSO

~5 mg/mL(warmed)

l  生物学信息

生物活性/药理作用

PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively. Acetyl CoA carboxylase (ACC) generates malonyl CoA, which is a substrate for de novo lipogenesis and is also an inhibitor of mitochondrial fatty acid β-oxidation through inihbition of carnitine-palmitoyl transferase I (CPT-1), responsible for the transport of long-chain fatty acyl-CoAs across the mitochondrial membrane. ACC inihibitors are hoped to inhibit de novo lipogenesis and increase β-oxidation of long-chain fatty acids with potential for treatment of type 2 diabetes, hepatic steatosis, and cancer. In Phase I clinical studies for diabetes treatment, PF-05175157 inhibited de novo lipogenesis and increased net whole-body fatty acid utilization.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.  https://www.ncbi.nlm.nih.gov