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Home / Biochemicals / Small Molecules

Sitaxsentan

SKU : BHB21300326

A Potent and Selective Antagonist of Endothelin A Receptor

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Mfr.No.	S-186, S-186_10 mg, S-186_25 mg, S-186_5 mg, S-186_50 mg
Description	Sitaxsentan (#S-186) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C18H15ClN2O6S2.
Synonyms	Synthetic
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 uM, 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.
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
Concentration	1-100 nM.
Reconstitution	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Cas Number	184036-34-8
Molecular Weight	454.9
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptors
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 uM, 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.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes 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.

Purity	>99% (HPLC)
Form	Lyophilized powder.
Storage	Storage After Reconstitution: 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. Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Wu, C. et al. (1997) J. Med. Chem. 40, 1690. Lepist, E.I. et al. (2014) PLoS One 9, e87548. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Wu, C. et al. (1997) J. Med. Chem. 40, 1690. Langleben, D. et al. (2004) Chest 126, 1377.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300326-1	S-186_10 mg	10 mg	$168		Add to Cart
BHB21300326-2	S-186_25 mg	25 mg	$219		Add to Cart
BHB21300326-3	S-186_5 mg	5 mg	$117		Add to Cart
BHB21300326-4	S-186_50 mg	50 mg	$366		Add to Cart

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