Macitentan

≥98% (HPLC)

Sinônimo(s):

ACT 064992, ACT-064992, ACT064992, Actelion-1, N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propyl-sulfamide

Sobre este item

Fórmula empírica (Notação de Hill):

C₁₉H₂₀Br₂N₆O₄S

Número CAS:

441798-33-0

Peso molecular:

588.27

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD17167076

Assay:

≥98% (HPLC)

Form:

powder

Propriedades

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

Descrição

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.