Aprocitentan
Cat. No.：YN321048
CAS No. ：1103522-45-7
| 产品名称: | Aprocitentan |
| CAS No.: | 1103522-45-7 |
| Chemical Name: | N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-sulfamide |
| Synonyms: | ACT-132577 |
| 分子量: | 546.19 |
| 分子式: | C₁₆H₁₄Br₂N₆O₄S |
| SMILES: | O=S(N)(NC1=NC=NC(OCCOC2=NC=C(Br)C=N2)=C1C3=CC=C(Br)C=C3)=O |
| 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: | Aprocitentan (ACT-132577) 是 Macitentan 的主要活性代谢物。Aprocitentan 是双重ETA/ETB拮抗剂，IC50分别为 3.4 nM 和 987 nM，pA2值分别为 6.7 和 5.5。 |
| IC50和靶点: | [{name:"ETA:3.4 nM (IC50)"},{name: "ETA:6.7 (pA2)"},{name: "ETB:987 nM (IC50)"},{name: "ETB:5.5 (pA2)"}] |
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Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al.Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin. Drug Saf.13(3),391-405(2013)
Iglarz, M., Binkert, C., Morrison, K., et al.Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonistJ. Pharmacol. Exp. Ther.327(3),736-745(2008)
Cutolo, M., Montagna, P., Brizzolara, R., et al.Effects of macitentan and its active metabolite on cultured human systemic sclerosis and control skin fibroblastsJ. Rheumatol.42(3),456-463(2015)
Trensz, F., Bortolamiol, C., Kramberg, M., et al.Pharmacological characterization of aprocitentan, a dual endothelin receptor antagonist, alone and in combination with blockers of the renin angiotensin system, in two models of experimental hypertensionJ. Pharmacol. Exp. Ther.368(3),462-473(2019)
