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ML-354
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。
ML-354图片
CAS NO:89159-60-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
ML-354 是一种选择性 PAR4 拮抗剂,IC50 为 140 nM。
Cas No.89159-60-4
别名VU0099704
化学名1-methyl-5-nitro-3-phenyl-1H-indole-2-methanol
Canonical SMILESCN1C(CO)=C(C2=CC=CC=C2)C3=C1C=CC([N+]([O-])=O)=C3
分子式C16H14N2O3
分子量282.3
溶解度≤2mg/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: 140 nM

ML-354 is an indole-based, proteinase-activated receptor (PAR) 4 antagonist with good potency and reasonable selectivity versus PAR1. PARs are a family of four G-protein-coupled receptors GPCRs (PAR1-PAR4) with several unique attributes, which are activated by serine proteases. The activation of PARs needs a unique mechanism which requiring proteolysis unmasking their extracellular N-terminal domain. PAR4 is a thrombin receptor found on human platelets and represents a potential therapeutic target for the treatment of thrombotic disorders [1].

In vitro: Up to now, in vitro study of ML-354 is still in the development stage.

In vivo: Up to now, in vivo study of ML-354 is still in the development stage.

Reference:
[1].  Wen, W., Young, S., Duvernay, M., Schulte, M., Nance, K., & Melancon, B. et al. Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354. Bioorganic & Medicinal Chemistry Letters. 2014; 24(19): 4708-4713.