Sitaxsentan

Product details

• Chemical name: N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide.
• Also known as: TBC-11251
• CAS number: 184036-34-8
• Molecular formula: C18H15ClN2O6S2.
• Purity: >99% (HPLC)
• Concentration: 1-100 nM.
• Form: Lyophilized powder.
• Solubility: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
• Reconstitution: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: ET-A receptors
• Source: Synthetic
• Activity: Sitaxsentan is a potent and selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to human ET-A and ET-B receptors with IC50 of 1.4 nM and 9.8 µM, respectively (a 7000-fold selectivity). in vitro, Sitaxsentan inhibits Endothelin-1 induced phosphoinositide turnover with a pA2 of 8.01. Sitaxsentan is orally bioavailable and active in vivo1,2.
• Alternative names: TBC-11251

Scientific background

Sitaxsentan, is a synthetic compound that acts as a potent and selective antagonist of ET-A endothelin receptors. Sitaxsentan is one of the most selective ET-A antagonists reported1. Sitaxsentan inhibits Endothelin-1 radioligand binding to human ET-A and ET-B receptors with IC50 values of 1.4 nM and 9.8 µM, respectively1.In pulmonary arterial hypertension clinical trials, sitaxsentan was shown to improve exercise capacity, improve functional capacity, and delay clinical worsening. However, the compound shows high liver toxicity and is no longer used to treat hypertension2.Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also distributed in several regions of the brain.ET-A has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity equally for all endothelin isopeptides3.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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