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Home / Biochemicals / Small Molecules

A-317491 sodium salt hydrate

SKU : BHB21300030

A Selective Antagonist of P2X3 and P2X2/3 Receptors

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Mfr.No.	A-380, A-380_10 mg, A-380_25 mg, A-380_5 mg, A-380_50 mg
Description	A-317491 sodium salt hydrate (#A-380) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C33H27NO8 + xNa + xH2O.
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.
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	50 nM - 50 uM.
Reconstitution	Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Cas Number	475205-49-3
Molecular Weight	565.57 (free acid, anhydrous)
Solubility	Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
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 uM1. This non-nucleotide antagonist reduces chronic inflammatory and neuropathic pain in the rat2.
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: 5-((3-phenoxyphenyl)methyl-((1S)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)benzene-1,2,4-tricarboxylic acid.

Purity	>98% (HPLC)
Form	Lyophilized Powder
Storage	Storage of solutions: -20°C.

Product Manual	SDS

Reference	Jarvis, M.F. et al. (2002) Proc. Natl. Acad. Sci. U.S.A. 99, 17179. Donnelly-Roberts, D. et al. (2008) J. Pharmacol. Exp. Ther. 324, 409. Pijacka, W. et al. (2016) Nat. Med. 22, 1151. Jarvis, M.F. et al. (2002) Proc. Natl. Acad. Sci. U.S.A. 99, 17179.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300030-1	A-380_10 mg	10 mg	$184		Add to Cart
BHB21300030-2	A-380_25 mg	25 mg	$417		Add to Cart
BHB21300030-3	A-380_5 mg	5 mg	$117		Add to Cart
BHB21300030-4	A-380_50 mg	50 mg	$645		Add to Cart

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