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Home / Biochemicals / Small Molecules

BMS 182874 hydrochloride

SKU : BHB21300068

A Selective Antagonist of Endothelin A Receptors

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Mfr.No.	B-500, B-500_10 mg, B-500_25 mg, B-500_5 mg, B-500_50 mg
Description	BMS 182874 hydrochloride (#B-500) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C17H19N3O3S · HCl
Background	BMS 182874 hydrochloride is a synthetic compound that acts as a selective, potent, and competitive antagonist of endothelin A (ET-A) receptors. BMS 182874 exhibits a 1000-fold selectivity for ET-A over ET-B receptors. The compound is a useful tool for understanding the role of endothelin in normal and disease conditions. BMS 182874 inhibits the binding of radioligand binding of ET-1 to ET-A receptors in rat vascular smooth muscle cell membranes with Ki of 61 nM and in Chinese ovary hamster cells with Ki of 48 nM1.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 where they mediate vasoconstriction. They are also expressed in several different regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides2.
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	100 nM - 10 uM.
Reconstitution	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
Cas Number	1215703-04-0
Molecular Weight	381.88
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptors
Source	Synthetic
Activity	BMS 182874 hydrochloride is a potent, selective and competitive antagonist of ET-A endothelin receptors. It exhibits a 1000-fold selectivity for ET-A over ET-B receptors, inhibiting endothelin-1 radioligand binding to ET-A and ET-B with Ki of 61 nM and >50 uM, respectively. In vitro, BMS 182874 inhibits endothelin-1 induced calcium mobilization with KB of 140 nM1. BMS 182874 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: 5-(dimethylamino)-N-(3,4-dimethyl-1,2-oxazol-5-yl)naphthalene-1-sulfonamide;hydrochloride.

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	Webb, M.L. et al. (1995) J. Pharmacol. Exp. Ther. 272, 1124. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Webb, M.L. et al. (1995) J. Pharmacol. Exp. Ther. 272, 1124. Holm, P. et al. (1998) Cardiovasc. Res. 37, 765.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300068-1	B-500_10 mg	10 mg	$134		Add to Cart
BHB21300068-2	B-500_25 mg	25 mg	$297		Add to Cart
BHB21300068-3	B-500_5 mg	5 mg	$85		Add to Cart
BHB21300068-4	B-500_50 mg	50 mg	$537		Add to Cart

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