Darusentan
Cat. No.：YN320976
CAS No. ：171714-84-4
| 产品名称: | Darusentan |
| CAS No.: | 171714-84-4 |
| Chemical Name: | αS-[(4,6-dimethoxy-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid |
| Synonyms: | Lu-135252 |
| 分子量: | 410.42 |
| 分子式: | C₂₂H₂₂N₂O₆ |
| SMILES: | COC1=NC(O[C@H](C(O)=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)=NC(OC)=C1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Darusentan (Lu-135252) 是一种选择性内皮素受体 A (ET-A) 受体拮抗剂，其与 ET-A 受体的Ki为 1.4 nM，与 ET-B 受体的 Ki为 184 nM，对 ETA 受体的选择性比 ETB 受体高100多倍。Darusentan 在大鼠主动脉血管平滑肌细胞 (RAVSMs) 膜中竞争结合放射性标记的内皮素，Ki为 13 nM。 |
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Liang, F., Glascock, C.B., Schafer, D.L., et al.Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteriesCan. J. Physiol. Pharmacol.88(8),840-849(2010)
Schiffrin, E.L., Turgeon, A., and Deng, L.Y.Effect of chronic ETA-selective endothelin receptor antagonism on blood pressure in experimental and genetic hypertension in ratsBr. J. Pharmacol.121(5),935-940(1997)
Gonon, A.T., Wang, Q.D., Shimizu, M., et al.The novel non-peptide selective endothelin A receptor antagonist LU 135 252 protects against myocardial ischaemic and reperfusion injury in the pigActa Physiol. Scand.163(2),131-137(1998)
