產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
BMS 309403 | 5mg 10mg 25mg | 300657-03-8 | EY-Y0163954 |
Cas No.300657-03-8
別名
化學名 2-((2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)-[1,1'-biphenyl]-3-yl)oxy)acetic acid
分子式 C31H26N2O3
分子量 474.55
溶解度 ≥ 18.15mg/mL in DMSO
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
BMS309403 is specifically designed to target FABP4 with a Ki value less than 2 nM. It is a potent and selective FABP4 inhibitor.[1]
Fatty acid binding proteins (FABPs) are small-molecular weight hydrophobic proteins containing a large hydrophobic cavity, into which naturally occurring long-chain fatty acids and synthetic hydrophobic ligands can be accepted. FABPs act as transporters of endogenous fatty acids from the cell surface to various sites of fatty acid storage and metabolism. In addition to the roles of FABP4 in regulating lipid metabolism and insulin sensitivity, recent pharmacological and biological ?ndings have indicated a regulatory function of FABP4 in in?ammation. FABP4 is expressed mainly to macrophages and in?ammatory response[1,2]
BMS309403 is an aromatic biphenyl azol compound that competes with fatty acids for the binding pocket of A-FABP with high speci?city. BMs30940323 has been shown to lower Mcp-1 secretion from thp-1 macrophages.[3,4]
Chronic administration of BMS309403 (15 mg/kg/day; from 12 to 18 weeks of age) in ApoE-/-mice signi?cantly improved therelaxations, maximal relaxation and EC50 to UK14304, acetylcholine and A23187. Mice orally BMS309403 significantly increased glucose uptake in myotubes in a time and dose dependent manner. Administered with BMS309403 are effectively protected against severe atherosclerosis and type 2 diabetes.[3,4]
References:
[1]Okada T, Hiromura M, Otsuka M etal. , Synthesis of BMS-309403-related compounds, including [1?C]BMS-309403, a radioligand for adipocyte fatty acid binding protein. Chem Pharm Bull (Tokyo). 2012;60(1):164-8.
[2]Suhre K, R?misch-Margl W, de Angelis MH etal. , Identification of a potential biomarker for FABP4 inhibition: the power of lipidomics in preclinical drug testing. J Biomol Screen. 2011 Jun;16(5):467-75
[3] Lin W1, Huang X, Zhang Letal. , BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase. PLoS One. 2012;7(8):e44570.
[4] Lee MY, Li H, Xiao Y, Zhou Z, Xu A, Vanhoutte PM. Chronic administration of BMS309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells. Br J Pharmacol. 2011 Apr;162(7):1564-76.
關鍵字： 300657-03-8;C31H26N2O3;BMS 309403;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務于科研工作者""的企業(yè)理念，立足生物科技領域，運用生物技術和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構、高等院校、科研院所、企事業(yè)單位提供優(yōu)質的產(chǎn)品，服務生物科技領域的科學研究人員。
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