ML-354 (Synonyms: VU0099704) |
Catalog No.GC15710 |
ML-354 es un antagonista selectivo de PAR4 con una IC50 de 140 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 89159-60-4
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
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