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Home / Biochemicals / Small Molecules

PD-156707

SKU : BHB21300279

A Potent and Selective Antagonist of Endothelin A Receptors

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Mfr.No.	P-305, P-305_10 mg, P-305_25 mg, P-305_5 mg, P-305_50 mg
Description	PD-156707 (#P-305) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C28H25O9·Na.
Background	PD-156707 is a synthetic compound that acts as a potent and selective antagonist of Endothelin A receptor (ET-A) subtype. PD-156707 is being used to define the physiological and pathological roles of endothelin A receptors. It demonstrates selectivity for ET-A receptor over ET-B receptor1,2.PD-156707 inhibits endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 0.17 nM and 133.8 nM, respectively1 and antagonizes endothelin-1-stimulated phosphoinositide hydrolysis in Ltk cells expressing cloned human endothelin A receptors with an IC50 value of 2.4 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 expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several regions of the brain. 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 equally high affinity 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	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	162412-70-6
Molecular Weight	528.49
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptor
Source	Synthetic
Activity	PD-156707 is a potent and selective antagonist of the ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 0.17 nM and 133.8 nM, respectively. in vitro, PD-156707 inhibits ET-A and ET-B receptor-mediated arterial vasoconstriction with pA2 of 7.5 and 4.7, respectively. PD-156707 is orally bioavailable and active in vivo1.
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: Sodium (Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-((3,4,5-trimethoxyphenyl)methyl)but-2-enoate.

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 of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Reynolds, E.E. et al. (1995) J. Pharmacol. Exp. Ther. 273, 1410. Maguire, J.J. et al. (1997) J. Pharmacol. Exp. Ther. 280, 1102. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Reynolds, E.E. et al. (1995) J. Pharmacol. Exp. Ther. 273, 1410.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300279-1	P-305_10 mg	10 mg	$134		Add to Cart
BHB21300279-2	P-305_25 mg	25 mg	$297		Add to Cart
BHB21300279-3	P-305_5 mg	5 mg	$85		Add to Cart
BHB21300279-4	P-305_50 mg	50 mg	$476		Add to Cart

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