ML-354

A PAR4 antagonist

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库存: 现货

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数量
1mg

￥537.00

430.00

- +
5mg

￥1450.00

1160.00

- +
10mg

￥2487.00

1990.00

- +
25mg

￥5787.00

4630.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci15662
CAS: 89159-60-4
别名: VU0099704
分子式: C16H14N2O3
分子量: 282.3
纯度: >98%
溶解度: ≤2mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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.