SML3386
Macitentan
≥98% (HPLC)
동의어(들):
ACT 064992, ACT-064992, ACT064992, Actelion-1, N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propyl-sulfamide
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C19H20Br2N6O4S
CAS Number:
Molecular Weight:
588.27
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
−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
생화학적/생리학적 작용
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.
신호어
Danger
유해 및 위험 성명서
Hazard Classifications
Repr. 1B
Storage Class Code
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
시험 성적서(COA)
Lot/Batch Number
Natalia Landázuri et al.
Cells, 10(11) (2021-11-28)
Human cytomegalovirus (HCMV) infection is an important cause of morbidity and mortality in immunocompromised patients and a major etiological factor for congenital birth defects in newborns. Ganciclovir and its pro-drug valganciclovir are the preferred drugs in use today for prophylaxis
Argen Mamazhakypov et al.
Pulmonary circulation, 10(4), 2045894020947283-2045894020947283 (2020-11-27)
Pulmonary arterial hypertension is a severe respiratory disease characterized by pulmonary artery remodeling. RV dysfunction and dysregulated circulating metabolomics are associated with adverse outcomes in pulmonary arterial hypertension. We investigated effects of tadalafil and macitentan alone or in combination on
Alexander Treiber et al.
Pharmacology research & perspectives, 8(4), e00619-e00619 (2020-07-03)
The dual endothelin receptor antagonist macitentan was approved in 2013 for the treatment of pulmonary arterial hypertension. Macitentan is an inducer of cytochrome P450 expression in vivo in animal species but not in man. In rat and dog, changes in
Soyoung Son et al.
Biomaterials, 276, 121058-121058 (2021-08-17)
Immune checkpoint therapy (ICT), which reinvigorates cytotoxic T cells, provides clinical benefits as an alternative to conventional cancer therapies. However, its clinical response rate is too low to treat an immune-excluded tumor, owing to the presence of abundant stromal elements
Xiaojian Gao et al.
Journal of proteome research, 19(8), 3302-3314 (2020-07-10)
Chronic mountain sickness (CMS) is a high altitude complication with high rates of morbidity and mortality. CMS is characterized by high-altitude polycythemia (HAPC) and high-altitude pulmonary hypertension (HAPH). In this study, macitentan, a dual endothelin receptor antagonist, was used to
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