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YM-254890

Chemical Structure : YM-254890

CAS No.: 568580-02-9

YM-254890 (YM254890)

Catalog No.: PC-62046Not For Human Use, Lab Use Only.

YM 254890 is a selective Gq signaling inhibitor that strongly inhibits intracellular calcium ion mobilization and serum response element (SRE)-mediated transcription stimulated by several receptors coupled to Gq, but not those coupled to Gi, Gs, or G15.

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Biological Activity

YM 254890 is a selective Gq signaling inhibitor that strongly inhibits intracellular calcium ion mobilization and serum response element (SRE)-mediated transcription stimulated by several receptors coupled to Gq, but not those coupled to Gi, Gs, or G15.
YM 254890 also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats.
YM 254890 inhibits ADP-induced platelet aggregation in human platelet-rich plasma with an IC50 of <0.6 uM by blocking the P2Y1 receptor-signal transduction pathway.

Physicochemical Properties

M.Wt 960.08
Formula C46H69N7O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1R)-1-((3S,9S,12S,18R,21S,22R)-21-acetamido-18-benzyl-3-((R)-1-methoxyethyl)-4,9,10,12,16,22-hexamethyl-15-methylene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentaazacyclodocosan-6-yl)-2-methylpropyl (2S,3R)-2-acetamido-3-hydroxy-4-methylpentan

References

1. Nishimura A, et al. Proc Natl Acad Sci U S A. 2010 Aug 3;107(31):13666-71.

2. Takasaki J, et al. J Biol Chem. 2004 Nov 12;279(46):47438-45.

3. Taniguchi M, et al. J Antibiot (Tokyo). 2003 Apr; 56(4):358-63.

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