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BM 567
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。
BM 567图片
CAS NO:284464-77-3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
dual acting antithrombogenic agent, acting as an inhibitor of thromboxane A2 (TXA2) synthase and as an antagonist of the TP receptor
Cas No.284464-77-3
化学名2-(cyclohexylamino)-5-nitro-N-[(pentylamino)carbonyl]-benzenesulfonamide
Canonical SMILESCCCCCNC(=O)NS(=O)(=O)c1cc(ccc1NC1CCCCC1)[N](=O)O
分子式C18H28N4O5S
分子量412.5
溶解度≤10mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
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

IC50: 1.1 nM for TXA2 receptor antagonism

BM 567 is acting as an inhibitor of thromboxane A2 (TXA2) synthase and an antagonist of the TP receptor.

Thromboxane A2 (TXA2), a potent thrombogenic and vasoconstrictor eicosanoid, is produced in large quantities by activated platelets. TXA2 has been reported as a causal factor in the onset of stroke and myocardial infarction.

In vitro: BM 567 was identified as a dual acting antithrombogenic agent, acting as an inhibitor of thromboxane A2 (TXA2) synthase and an antagonist of the TP receptor, the G protein-coupled receptor mediating TXA2 activity in platelets and vascular smooth muscle. BM 567 antagonized the vascular smooth muscle TP receptor with an IC50 value of 1.1 nM. BM 567 was also able to inhibit platelet TX synthase with an IC50 value of 12 nM. In addition, by comparing crystallographic and electronic properties of BM567 and terbogrel, two compounds with dual action (TXRA and TXSI), two essential anchoring identified: sulfonyl and nitro group for BM567 and carboxylate and pyridine nitrogen for terbogrel [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Michaux, C. ,Rolin, S.,Dogné, J.M., et al. Structure determination and comparison of BM567, a sulfonylurea, with Terbogrel, two compounds with dual action, thromboxane receptor antagonism, and thromboxane synthase inhibition. Bioorganic & Medicinal Chemistry Letters 11, 1019-1022 (2001).