A-317491 sodium salt hydrate

Product details

• Chemical name: 5-[(3-phenoxyphenyl)methyl-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]benzene-1,2,4-tricarboxylic acid.
• CAS number: 475205-49-3
• Molecular formula: C33H27NO8 + xNa + xH2O.
• Molecular weight: 565.57 (free acid, anhydrous)
• Purity: >98% (HPLC)
• Concentration: 50 nM - 50 µM.
• Form: Lyophilized Powder
• Solubility: Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• 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: P2X3 receptors
• Source: Synthetic
• Activity: A-317491 sodium salt hydrate is a selective antagonist of the P2X3 and P2X2/3 receptors. It was shown to inhibit human homomeric P2X3 and heteromeric P2X2/3 receptors with pIC50 values of ~7, whilst exhibiting little to no antagonistic activity on other P2X family receptors, and no effect on P2Y2 at over 10 µM1. This non-nucleotide antagonist reduces chronic inflammatory and neuropathic pain in the rat2.

Scientific background

A-317491 is a selective, competitive, non-nucleotide antagonist of P2X3 and P2X2/3 receptors. It is shown to inhibit human homomeric P2X3 and heteromeric P2X2/3 receptors with pIC50 values of ~7 and exhibits almost no antagonistic activity on other P2X family receptors1. The compound is active in chronic inflammatory and neuropathic pain models, but is ineffective in reducing nociception in animal models of acute, postoperative, and visceral pain.A-317491 is the chiral pure S-enantiomer, while the R-enantiomer, A-317344, shows lower activity at P2X3 and P2X2/3 receptors in vitro and lacks anti-nociceptive effects in animal models. A-317491 shows high systemic bioavailability following subcutaneous administration but lacks oral bioavailability. It is not susceptible to metabolic degradation1,2.P2X receptors are a family of ion channels gated by ATP. They are expressed in cell types of almost every origin, including neuronal, muscular, epithelial and immune and have been shown to play a pivotal role in models of various pain conditions3.

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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