ML-354 (Synonyms: VU0099704) |
| Katalog-Nr.GC15710 |
ML-354 ist ein selektiver PAR4-Antagonist mit einem IC50 von 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.
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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 (Based on Reviews and 37 reference(s) in Google Scholar.)
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