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CAS No. : 1103522-45-7
MCE 国际站:Aprocitentan
产品活性: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。
研究领域:GPCR/G Protein
作用靶点:Endothelin Receptor
In Vitro: Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell line A10 and mouse fibroblast cell line 3T3).
In Vivo: Aprocitentan (ACT-132577) has a volume of distribution greater than the plasma volume and a longer half-life than its parent compound in the rat. In rat plasma, the mean recovery of Aprocitentan (ACT-132577) ranges from 82.6% to 90.6%, matrix effect of Aprocitentan (ACT-132577) in rat plasma ranges from 101.4% to 115.2%.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cardiovascular Disease Compound Library | Endocrinology Compound Library | Orally Active Compound Library | Neurotransmitter Receptor Compound Library | Angiogenesis-Related Compound Library | Targeted Diversity Library | Coagulation and Anti-coagulation Compound Library | Pain-Related Compound Library | Antihypertensive Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | BQ-788 | [Asn18] Endothelin-1, human | TBC3711 | BQ-3020 TFA | Sparsentan | [Lys4] Sarafotoxin S6c | Nebentan potassium | Bosentan | Endothelin 1 (swine, human) (TFA) | Ambrisentan | Ro 46-2005 | [Ala2] Endothelin-3, human | ZD-1611 | PD-159020 | Aminaftone | A-192621 | Macitentan | Sulfisoxazole | Endothelin-3, human, mouse, rabbit, rat TFA | IRL 2500 | Carperitide acetate | Atrial Natriuretic Peptide (ANP) (1-28), rat TFA | ACT-373898 | Kendomycin | Zibotentan | BQ-123 TFA
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