A cyclic depsipeptide Gαq/11 inhibitor
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YM-254890

Item No. 29735

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-L-threonine(7→1)-lactone
CAS Number
568580-02-9
Molecular Formula
C46H69N7O15
Formula Weight
960.1
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
SMILES
O=C(N[C@@H](C)C1=O)C(N(C)C([C@H](OC([C@@H](NC(C)=O)[C@H](OC([C@@]([C@@H](C)OC)([H])N(C)C([C@@]([C@@H](C(C)C)OC([C@H]([C@H](O)C(C)C)NC(C)=O)=O)([H])NC([C@@H](N1C)C)=O)=O)=O)C)=O)CC2=CC=CC=C2)=O)=C
InChi Code
InChI=1S/C46H69N7O15/c1-22(2)37(56)34(49-30(11)55)45(63)68-38(23(3)4)35-43(61)53(14)36(28(9)65-15)46(64)66-27(8)33(48-29(10)54)44(62)67-32(21-31-19-17-16-18-20-31)42(60)52(13)25(6)39(57)47-24(5)41(59)51(12)26(7)40(58)50-35/h16-20,22-24,26-28,32-38,56H,6,21H2,1-5,7-15H3,(H,47,57)(H,48,54)(H,49,55)(H,50,58)/t24-,26-,27+,28+,32+,33-,34-,35-,36-,37+,38+/m0/s1
InChi Key
QVYLWCAYZGFGNF-WBWCVGBTSA-N
Origin
Bacterium/Chromobacterium sp
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $369

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    Product Description

    YM-254890 is cyclic depsipeptide originally isolated from Chromobacterium and an inhibitor of Gαq/11.1 It inhibits Gαq/11-mediated intracellular calcium mobilization induced by 2MeSADP or methacholine in C6-15 cells expressing the purinergic P2Y1 receptor (IC50 = 0.15 µM) and in CHO cells expressing M1 muscarinic acetylcholine receptors (IC50 = 0.15 µM), respectively, but has no effect on Gαi-mediated calcium mobilization induced by fMLP in HL-60 cells (IC50 = >10 µM). YM-254890 inhibits platelet aggregation induced by ADP, collagen, thrombin receptor agonist peptide (TRAP), arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), or U-46619 (Item No. 16450) in isolated human platelet-rich plasma (IC50s = 0.39, 0.15, 0.71, 0.25, and 0.34 µM, respectively).2 It reduces shear stress-induced thrombus formation in isolated human whole blood. YM-254890 (1, 3, and 10 µg/kg) reduces platelet thrombus formation in a cynomolgus monkey model of femoral artery thrombosis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takasaki, J., Saito, T., Taniguchi, M., et al. A Novel Gɑq/11-selective Inhibitor. The Journal of Biological Chemisty 279(46), 47438-47445 (2004).

    2. Uemura, T., Kawasaki, T., Taniguchi, M., et al. Biological properties of a specific Gɑq/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress. Br. J. Pharmacol. 148(1), 61-69 (2006).