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BMY 45778
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BMY 45778图片
CAS NO:152575-66-1
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
partial agonist at IP1 prostacyclin receptors
Cas No.152575-66-1
化学名2-(3-(4,5-diphenyl-[2,4'-bioxazol]-5'-yl)phenoxy)acetic acid
Canonical SMILESOC(COC1=CC(C2=C(C3=NC(C4=CC=CC=C4)=C(C5=CC=CC=C5)O3)N=CO2)=CC=C1)=O
分子式C26H18N2O5
分子量438.44
溶解度<21.92mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BMY 45778 is a partial agonist of prostacyclin receptor [1].

Prostacyclin receptor (IP1) is a G-protein coupled receptor for prostacyclin. Prostacyclin inhibits platelet aggregation and elicits a potent vasodilation through binding to this receptor.

BMY 45778 is a partial agonist of prostacyclin receptor. BMY 45778 inhibited platelet aggregation with IC50 values of 35 nM, 136 nM and 1.3 μM in human, rabbit and rat, respectively. In human platelet membrane, BMY 45778 activated adenylyl cyclase with ED50 value of 6-10 nM and stimulated GTPase. Also, BMY 45778 completely inhibited the binding of Iloprost to platelet membranes with IC50 value of 7 nM. BMY 45778 inhibited iloprost-stimulated GTPase, which suggested that BMY 45778 is a partial agonist of prostacyclin receptor. In whole platelets, BMY 45778 increased cAMP levels and activated cAMP-dependent protein kinase [1]. BMY 45778 (1-10 μM) inhibited rat neutrophil aggregation induced by N-formyl-methionyl-leucylphenylalanine with IC50 value of 20 nM and inhibited the spontaneous activity of rat colon by 10-20%. Also, BMY 45778(10 μM) inhibited the inhibitory effect of cicaprost on rat colon [2].

References:
[1].  Seiler SM, Brassard CL, Federici ME, et al. [3-[4-(4,5-Diphenyl-2-oxazolyl)-5-oxazolyl]phenoxy]acetic acid (BMY 45778) is a potent non-prostanoid prostacyclin partial agonist: effects on platelet aggregation, adenylyl cyclase, cAMP levels, protein kinase, and iloprost binding. Prostaglandins, 1997, 53(1): 21-35.
[2].  Wise H, Qian YM, Jones RL. A study of prostacyclin mimetics distinguishes neuronal from neutrophil IP receptors. Eur J Pharmacol, 1995, 278(3): 265-269.