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Biochem/physiol Actions
Macitentan (ACT-064992; actelion-1) is an orally active, potent endothelin (ET) receptor antagonist that blocks ET-1-induced cellular calicum response (IC50 in nM = 0.9/HPASMC, 0.8/RASMC, 1.84/m3T3), as well as ET-1-induced contractions of rat aortic rings (ETA) and S6c-induced rat tracheal rings (ETB) ex vivo (pA2 = 7.6 and 5.9, respectively). Macitentan displays therapeutic efficacy in rat hypertension models in vivo (0.3-100 mg/kg p.o. via single or daily dosing).
Orally active, potent endothelin (ET) receptor antagonist with therapeutic efficacy against hypertension in vivo.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | BrC1=CC=C(C=C1)C2=C(N=CN=C2OCCOC3=NC=C(C=N3)Br)NS(NCCC)(=O)=O |
| InChI | 1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27) |
| InChI key | JGCMEBMXRHSZKX-UHFFFAOYSA-N |
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