推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
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 key
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).
Orally active, potent endothelin (ET) receptor antagonist with therapeutic efficacy against hypertension in vivo.
警示用语：
Danger
危险声明
危险分类
Repr. 1B
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
Hao-Chen Liu et al.
Acta pharmacologica Sinica, 41(5), 719-728 (2020-01-15)
Sunitinib is an oral small molecule multitargeted tyrosine kinase inhibitor, which is currently used to treat severe cancers. Clinical research has shown that patients treated with sunitinib develop hypertension. As soon as sunitinib-induced hypertension appears, it is usual to administer
Philipp Baumann et al.
Journal of translational medicine, 20(1), 77-77 (2022-02-07)
Cardiovascular impairment contributes to increased mortality in preterm infants with chronic lung disease. Macitentan, an endothelin-1 receptor antagonist, has the potential to attenuate pulmonary and cardiovascular remodelling. In a prospective randomized placebo-controlled intervention trial, Sprague-Dawley rats were exposed to 0.21
Marc Iglarz et al.
The Journal of pharmacology and experimental therapeutics, 327(3), 736-745 (2008-09-11)
Macitentan, also called Actelion-1 or ACT-064992 [N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N'-propylaminosulfonamide], is a new dual ET(A)/ET(B) endothelin (ET) receptor antagonist designed for tissue targeting. Selection of macitentan was based on inhibitory potency on both ET receptors and optimization of physicochemical properties to achieve high
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
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