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Home / Biochemicals / Small Molecules

PD-164333

SKU : BHB21300280

A Selective Antagonist of Endothelin A Receptors

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Mfr.No.	P-310, P-310_0.5 mg, P-310_1 mg, P-310_2.5 mg, P-310_5 mg
Description	PD-164333 (#P-310) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C39H38INO11.
Background	PD-164333 is a synthetic compound that acts as a selective antagonist of ET-A endothelin receptor based on the butenolide series1. It inhibits the binding of radioligand endothelin-1 to left ventricle in a biphasic manner with a KD value of 0.99 nM and 2.41 uM towards ET-A and ET-B, respectively1.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 different regions of the brain. ET-A receptor has a 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 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	1-100 nM.
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	1027525-70-7
Molecular Weight	823.63
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptors
Source	Synthetic
Activity	PD-164333 is a selective antagonist of the ET-A receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Kd of 0.99 nM and 2.41 uM, respectively. in vitro, PD164333 shifts Endothelin-1 concentration-response curve to the right with pA2 of 8.84 in isolated human saphenous vein1.
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: (Z)-2-(1,3-benzodioxol-5-yl)-3-((3-(4-(2-(4-hydroxy-3-iodophenyl)ethylamino)-4-oxobutoxy)-4,5-dimethoxyphenyl)methyl)-4-(4-methoxyphenyl)-4-oxobut-2-enoic acid.

Purity	>98%
Form	Lyophilized powder.
Storage	Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Davenport, A.P. et al. (1998) Br. J. Pharmacol. 123, 223. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Davenport, A.P. et al. (1998) Br. J. Pharmacol. 123, 223.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300280-1	P-310_0.5 mg	0.5 mg	$168		Add to Cart
BHB21300280-2	P-310_1 mg	1 mg	$287		Add to Cart
BHB21300280-3	P-310_2.5 mg	2.5 mg	$502		Add to Cart
BHB21300280-4	P-310_5 mg	5 mg	$680		Add to Cart

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