This product has recently been released.
This product is freeze dried. All water molecules have been removed.
The activity of this product has been verified and approved by our professional team.
This lyophilized product is shipped at room temperature. Please see its certificate of analysis for further storage instructions.
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 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 is pleased to offer Sitaxsentan sodium salt (#S-185).
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