chemical

Sitaxsentan

S-186

S-186_10 mg

Sitaxsentan

Non Antibodies

S. Molecules

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

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

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.

Alomone Labs

ET-A receptors

Sitaxsentan (#S-186) is a highly pure, synthetic, and biologically active compound.

A Potent and Selective Antagonist of Endothelin A Receptor

454.9

TBC-11251

Synthetic

C18H15ClN2O6S2.

1-100 nM.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1-2 Business Days

Israel/IL

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.

>99% (HPLC)

184036-34-8

Lyophilized powder.

Contact Alomone Labs for technical support and product customization

41116134

Yes

N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide.