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PZ0203

Sigma-Aldrich

Sitaxentan sodium salt

≥98% (HPLC)

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C18H14ClN2NaO6S2
Numéro CAS:
210421-74-2
Poids moléculaire :
476.89
Code UNSPSC :
51111800
ID de substance PubChem :
329823772
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

H2O: 10 mg/mL (clear solution)

Température de stockage

room temp

Chaîne SMILES 

[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

Clé InChI

MDTNUYUCUYPIHE-UHFFFAOYSA-N

Informations sur le gène

human ... EDNRA(1909) , EDNRB(1910)

Actions biochimiques/physiologiques

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.
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).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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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)
Christian Garcia-Abrego et al.
International journal of molecular sciences, 21(17) (2020-09-06)
Hematopoietic stem/progenitor cells (HSPCs) are responsible for the generation of blood cells throughout life. It is believed that, in addition to soluble cytokines and niche cells, biophysical cues like elasticity and oxygen tension are responsible for the orchestration of stem
Hagai Tavori et al.
Journal of lipid research, 56(3), 635-643 (2015-01-17)
Tissue cholesterol accumulation, macrophage infiltration, and inflammation are features of atherosclerosis and some forms of dermatitis. HDL and its main protein, apoAI, are acceptors of excess cholesterol from macrophages; this process inhibits tissue inflammation. Recent epidemiologic and clinical trial evidence
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
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
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