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Home / Biochemicals / Small Molecules

Darusentan

SKU : BHB21300126

A Selective Antagonist of Endothelin A Receptors

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Mfr.No.	D-265, D-265_10 mg, D-265_25 mg, D-265_5 mg, D-265_50 mg
Description	Darusentan (#D-265) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C22H22N2O6.
Synonyms	Synthetic
Background	Darusentan, (LU 135252), is a synthetic compound that acts as a selective antagonist of endothelin A (ET-A) receptors. Darusentan is orally bioavailable and is a potent inhibitor of vasoconstriction in large and small arteries. The compound is a propanoic acid based antagonist that consist of two enantiomers - (R) and (S). The (R) enantiomer shows no binding activity, indicating that the (S) enantiomer is the active drug1,2.in vitro, Darusentan inhibits endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 value of 8.11,2.Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also detected in several different regions of the brain3.
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 nM - 1 uM.
Reconstitution	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Cas Number	171714-84-4
Molecular Weight	410.43
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptors
Activity	Darusentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 6 nM and 371 nM, respectively1. in vitro Darusentan inhibits Endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 of 8.12. Darusentan is orally bioavailable and active in vivo3.
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: (2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid.

Purity	>99%
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 before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Liang, F. et al. (2010) Can. J. Physiol. Pharmacol. 88, 840. Enseleit, F. et al. (2010) Ther. Adv. Cardiovasc. Dis. 4, 231. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Riechers, H. et al. (1996) J. Med. Chem. 39, 2123. Liang, F. et al. (2010) Can. J. Physiol. Pharmacol. 88, 840. Prié, S. et al. (1997) J. Pharmacol. Exp. Ther. 282, 1312.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300126-1	D-265_10 mg	10 mg	$337		Add to Cart
BHB21300126-2	D-265_25 mg	25 mg	$595		Add to Cart
BHB21300126-3	D-265_5 mg	5 mg	$235		Add to Cart
BHB21300126-4	D-265_50 mg	50 mg	$917		Add to Cart

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