YM-254890
Modify Date: 2024-01-15 19:45:47
YM-254890 structure
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Common Name | YM-254890 | ||
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| CAS Number | 568580-02-9 | Molecular Weight | 960.078 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 1232.4±65.0 °C at 760 mmHg | |
| Molecular Formula | C46H69N7O15 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 699.1±34.3 °C | |
Use of YM-254890YM 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; also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats; 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. Thrombosis Discontinued |
| Name | [(1R)-1-[(3S,6S,9S,12S,18R,21S,22R)-21-acetamido-18-benzyl-3-[(1R)-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-pentazacyclodocos-6-yl]-2-methyl-propyl] (2S,3R)-2-acetamido-3-hydroxy-4-methyl-pentanoate |
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| Synonym | More Synonyms |
| Description | 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; also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats; 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. Thrombosis Discontinued |
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| Related Catalog | |
| Target |
Gαq/11 protein[1][2] |
| In Vitro | YM-254890 inhibits platelet aggregation induced by ADP (2, 5 and 20 μM) in human platelet-rich plasma with IC50 values of 0.37, 0.39 and 0.51 μM. ADP mediates platelet aggregation via two G protein-coupled receptors, P2Y1 and P2Y12. The effect of YM-254890 on the P2Y1 and P2Y12 signal transduction pathways using C6-15 cells stably expressing the human P2Y1 or P2Y12 receptors is examined. Stimulation of P2Y1-C6-15 cells by 2MeSADP leads to increases in intracellular calcium mobilization. In this assay, YM-254890 inhibits the increase in [Ca2+]i with an IC50 value of 0.031 μM. In contrast, 2MeSADP-induced inhibition of forskolin-stimulated adenylyl cyclase activity in P2Y12-C6-15 cells is unaffected by YM-254890 at 40 μM[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 1232.4±65.0 °C at 760 mmHg |
| Molecular Formula | C46H69N7O15 |
| Molecular Weight | 960.078 |
| Flash Point | 699.1±34.3 °C |
| Exact Mass | 959.485168 |
| LogP | -1.84 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.560 |
| Hazard Codes | Xi |
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| MFCD09832722 |