A 317491 sodium salt
Tocris Bioscience, part of Bio-Techne | Catalog # 6493
Selective, high affinity P2X3 and P2X2/3 antagonist; antinociceptive
Key Product Details
Description
Selective, high affinity P2X3 and P2X2/3 antagonist; antinociceptive
Product Description
A 317491 sodium salt is a 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.Product Specifications
Molecular Weight
609.54
Formula
C33H25NO8Na2
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
5-[[[(3-Phenoxyphenyl)methyl][(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]carbonyl]-1,2,4-benzenetricarboxylic acid disodium salt
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]
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 60.95 | 100 |
Preparing Stock Solutions
for A 317491 sodium salt
The following data is based on the product molecular weight 609.54
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.64 mL | 8.20 mL | 16.41 mL |
| 5 mM | 0.33 mL | 1.64 mL | 3.28 mL |
| 10 mM | 0.16 mL | 0.82 mL | 1.64 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.33 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Neelands 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. 2003 PMID: 12967950
- Mansoor X-ray structures define human P2X3 receptor gating cycle and antagonist action. Nature 2016 PMID: 27626375
- McGaraughty 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. 2003 PMID: 14623769
- McGaraughty 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. 2005 PMID: 16041397
- Jarvis 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 2002 PMID: 12482951
Product Specific Notices for A 317491 sodium salt
For research use only
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