PZ0203
Sitaxentan sodium salt
≥98% (HPLC)
别名:
N-(4-Chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonamide sodium salt, Sitaxsentan sodium salt, TBC-11251 sodium salt, Thelin
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
H2O: 10 mg/mL (clear solution)
储存温度
room temp
SMILES字符串
[Na+].Cc1cc2OCOc2cc1CC(=O)c3sccc3S(=O)(=O)[N-]c4onc(C)c4Cl
InChI
1S/C18H14ClN2O6S2.Na/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18;/h3-5,7H,6,8H2,1-2H3;/q-1;+1
InChI key
MDTNUYUCUYPIHE-UHFFFAOYSA-N
基因信息
human ... EDNRA(1909), EDNRB(1910)
生化/生理作用
Sitaxentan (Sitaxsentan) is a potent and selective endothelin ET(A) receptor antagonist once used in the treatment of pulmonary arterial hypertension (PAH), but removed from the market because of hepatotoxicity. It is over 6000-fold selective for the the ETA receptor subtype with an IC50 of 1 nM for ETA versus an IC50 of 9800 nM for ETB.
Sitaxentan is a potent and selective endothelin ET(A) receptor antagonist; antihypertensive.
Sitaxsentan prevents shunt mediated elevation of pulmonary vascular resistance (PVR). Sitaxsentan effectively inhibits basolateral Na+-taurocholate cotransporting polypeptide (NTCP), organic anion-transporting polypeptides (OATPs) and bile salt export pump (BSEP).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Wei Zhao et al.
OncoTargets and therapy, 11, 6071-6080 (2018-10-03)
Non-small-cell lung cancer (NSCLC) is the one of the most common malignancies worldwide, and occurs at a higher frequency in male individuals. Little is known about the role of the long intergenic noncoding RNA for kinase activation (LINK-A) in NSCLC
Jaroslav Řeháček et al.
Scientific reports, 5, 12289-12289 (2015-07-22)
We reveal that quadrature squeezing can result in significantly better quantum-estimation performance with quantum heterodyne detection (of H. P. Yuen and J. H. Shapiro) as compared to quantum homodyne detection for Gaussian states, which touches an important aspect in the
Shihab Shamma et al.
The Journal of the Acoustical Society of America, 145(2), 615-615 (2019-03-03)
Pitch is a fundamental attribute in auditory perception involved in source identification and segregation, music, and speech understanding. Pitch percepts are intimately related to harmonic resolvability of sound. When harmonics are well-resolved, the induced pitch is usually salient and precise
Srinivas Akula et al.
Cells, 9(1) (2020-01-18)
Mast cells (MCs) are primarily resident hematopoietic tissue cells that are localized at external and internal surfaces of the body where they act in the first line of defense. MCs are found in all studied vertebrates and have also been
Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes
Lepist EI, et al.
PLoS ONE, 9(1), e87548-e87548 (2014)
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