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A 317491 sodium salt

Catalog No.GC50474

Selective, high affinity P2X3 and P2X2/3 receptor antagonist; antinociceptive

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A 317491 sodium salt Chemical Structure

Size Price Stock Qty
5 mg
$226.00
In stock
25 mg
$883.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Selective, high affinity non-nucleotide P2X3 and P2X2/3 receptor antagonist (Ki values are 9, 22, 22 and 92 nM at human P2X2/3, rat P2X3, human P2X3 and rat P2X2/3, respectively); blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22 - 92 nM). Exhibits selectivity over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes (IC50 > 5 μM). Reduces mechanical allodynia and thermal hyperalgesia in the CCI in vivo models. Antinociceptive.

Jarvis et al (2002) A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc.Nat.Acad.Sci.USA 99 17179 PMID:12482951 |McGaraughty et al (2003) Effects of A-317491, a novel and selective P2X3/P2X2/3 receptor antagonist, on neuropathic, inflammatory and chemogenic nociception following intrathecal and intraplantar administration. Br.J.Pharmacol. 140 1381 PMID:14623769 |McGaraughty et al (2005) Endogenous opioid mechanisms partially mediate P2X3/P2X2/3-related antinociception in rat models of inflammatory and chemogenic pain but not neuropathic pain. Br.J.Pharmacol. 146 180 PMID:16041397 |Mansoor et al (2016) X-ray structures define human P2X3 receptor gating cycle and antagonist action. Nature 538 66 PMID:27626375 |Neelands et al (2003) 2', 3'-O-(2,4,6,trinitrophenyl)-ATP and A-317491 are competitive antagonists at a slowly desensitizing chimeric human P2X3 receptor. Br.J.Pharmacol. 140 202 PMID:12967950

Chemical Properties

Cas No. SDF
Canonical SMILES O=C(C1=CC(C(O)=O)=C(C(N([C@H]2CCCC3=CC=CC=C23)CC4=CC(OC5=CC=CC=C5)=CC=C4)=O)C=C1C(O[Na])=O)O[Na]
Formula C33H25NO8Na2 M.Wt 609.54
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.6406 mL 8.2029 mL 16.4058 mL
5 mM 0.3281 mL 1.6406 mL 3.2812 mL
10 mM 0.1641 mL 0.8203 mL 1.6406 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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