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Merck
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SML3386

Sigma-Aldrich

Macitentan

≥98% (HPLC)

同義詞:

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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About This Item

經驗公式(希爾表示法):
C19H20Br2N6O4S
CAS號碼:
分子量::
588.27
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

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 密鑰

JGCMEBMXRHSZKX-UHFFFAOYSA-N

生化/生理作用

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).

象形圖

Health hazard

訊號詞

Danger

危險聲明

危險分類

Repr. 1B

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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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
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
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
Chan-Hyeong Lee et al.
Theranostics, 12(5), 1971-1987 (2022-03-11)
Extracellular vesicles (EVs) carrying tumor cell-derived programmed death-ligand 1 (PD-L1) interact with programmed death 1 (PD-1)-producing T cells, thus significantly lowering a patient's response to immune checkpoint blockade drugs. No drug that reinvigorates CD8+ T cells by suppressing EV PD-L1

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