|2-(5-乙基-3,4-二苯基-吡唑-1-基)-联苯-3-基氧基]乙酸|CsnPharm

CAS No.: 300657-03-8

BMS-309403 Catalog No. CSN22610

Synonyms: Adipocyte FABP Inhibitor;A-FABP Inhibitor;ALBP Inhibitor

BMS-309403 is an inhibitor of fatty acid binding protein 4 (FABP4) with Ki of less than 2 nM that decreases fatty acid uptake in adipocytes in vitro.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Adipocyte fatty acid binding protein (aFABP) is a 14.6 kDa cytosolic protein located in adipocytes and macrophages, and assists in the intracellular transport of fatty acids. It is one of a class of fatty acid binding proteins (FABPs) that are found predominately in the liver, heart, intestine, and connective tissues^[5]. BMS-309403 is a potent, selective and cell-permeable inhibitor of FABP4 with a K_i of less than 2 nM, which exhibits K_i values 250 nM for FABP3 and 350 nM for FABP5^[5]. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. Treatment with BMS-309403 significantly decreased MCP-1 production from THP-1 macrophages in a dose- and time-dependent manner^[6]. BMS-309403 stimulates glucose uptake in C2C12 myotubes in a temporal and dose dependent manner via activation of AMP-activated protein kinase (AMPK) signaling pathway but independent of FABPs^[7]. The extent of atherosclerotic lesion area in the proximal aorta is significantly reduced in the BMS-309403-treated group compared with vehicle-treated controls in both the early and late intervention studies^[6]. A 6 weeks treatment with BMS-309403 improves endothelial function, phosphorylated and total eNOS (endothelial nitric oxide synthase) and reduced plasma triglyceride levels. In cultured human microvascular endothelial cells, lipid-induced aFABP expression is associated with reduced phosphorylated eNOS and NO production and is reversed by BMS-309403^[8].

动物研究

剂量

Mice: 40 mg/kg, 100 mg/kg^[1] (p.o.); 3 mg/kg - 30 mg/kg^[2] (p.o.) ; 1 mg/kg^[3] (i.p.) Rat: 5 mg/kg^[4] (i.p.)

给药途径

p.o., i.p.

动物药代数据

Animal	Mice^[1]
Dose	40 mg/kg
Administration	p.o.
C_max	5880 nM
T_max	0.67 h
AUC	23300 nM·h

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1073 mL
- 10.5363 mL
- 21.0726 mL
- 5 mM
- 0.4215 mL
- 2.1073 mL
- 4.2145 mL
- 10 mM
- 0.2107 mL
- 1.0536 mL
- 2.1073 mL

技术信息

CAS号

300657-03-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H26N2O3

运输

蓝冰

分子量

474.55

别名

Adipocyte FABP Inhibitor;A-FABP Inhibitor;ALBP Inhibitor;aP2 Inhibitor;FABP4 Inhibitor;Fatty Acid Binding Protein 4 Inhibitor

溶解度

DMSO	310.0 mg/mL (653.3 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

BMS-309403 Catalog No. CSN22610

靶点选择性

请登录您的专属账户

确认信息