PD-164333

SKU:BHB21300280
Overview
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PD-164333 (CAS 1027525-70-7) 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 µM, respectively. Supplied as Lyophilized powder (purity >98%, solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min)). Commonly used in Molecular & Cellular Biology studies, including binding assays and second-messenger readouts.
Target ET-A receptor
Cas No 1027525-70-7
concentration 1-100 nM.
purity >98%
Molecular Formula C39H38INO11.
Form Lyophilized powder.
Options selector
Catalog no. Size Quantity
P-310-0P5MG-1 0.5 mg
P-310-1MG-1 1 mg
P-310-2P5MG-1 2.5 mg
P-310-5MG-1 5 mg
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size (4) - 0.5 mg, 1 mg, 2.5 mg, 5 mg; Quantity: 1
  • Lead time: typically ships in 1-2 business days; timing may vary by selected option.
  • Storage: Storage of solutions: Up to three months at -20°C.
  • 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.
  • Upon receipt: store at the recommended temperature as soon as possible.
  • Sales terms and conditions: Please review prior to ordering.
Field Specification
Target ET-A receptor
CAS no. 1027525-70-7
Applications
  • Functional Assay (In Vitro)
Source Synthetic
Molecular formula C39H38INO11.
Purity >98%
Activity
  • Antagonist
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
Solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Concentration 1-100 nM.
Form Lyophilized powder.
Storage Storage of solutions: Up to three months at -20°C.
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.
Catalog no. (Mfr.) P-310
Main SKU BHB21300280

Product details

  • 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.
  • CAS number: 1027525-70-7
  • Molecular formula: C39H38INO11.
  • Purity: >98%
  • 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 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 µM, respectively. in vitro, PD164333 shifts Endothelin-1 concentration-response curve to the right with pA2 of 8.84 in isolated human saphenous vein1.

Scientific 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 µM 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.

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

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  • Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
  • QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
  • Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity

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