PD-156707

Product details

• Chemical name: Sodium (Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoate.
• CAS number: 162412-70-6
• Molecular formula: C28H25O9·Na.
• Purity: >99%
• Concentration: 1-100 nM.
• Form: Lyophilized powder.
• Solubility: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
• 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 µM - 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
• 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.
• 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.

Scientific 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.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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