A-317491 sodium salt hydrate
Based on 5 publication(s) in Google Scholar
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
For research use only. We do not sell to patients.
- Purity: 99.88%
- Formula: C33H29NNaO9
- Molecular Weight:606.57
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) A-317491 sodium salt hydrate
More
Customer Validation & Images
-
IF
All P2X Receptor Isoforms
More
Biological Activity
|
P2X3 Receptor |
A-317491 potently blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki=22-92 nM) [1].
A-317491 (1 nM-10 μM) produces a concentration-dependent block of dorsal root ganglion (DRG) currents with an IC50 of 15 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
A-317491 (3-30 mg/kg; a single .v.) exhibits the plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant[2]
-
Dosage:0.1, 1, 3, 10, 30 mg/kg
-
Administration:A single s.c.
-
Result:Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration.
Chemical Information
-
Appearance Solid
-
Molecular Weight 606.57
-
Formula C33H29NNaO9
-
Color White to off-white
-
SMILES
O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O.[Na].O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Research (Wash D C)
2025 Oct 20:8:0932. PMID: 41122266 -
Int J Nanomedicine
2017 Nov 9:12:8171-8183. PMID: 29184406
A-317491 sodium salt hydrate purchased from MedChemExpress. Usage Cited in: Int J Nanomedicine. 2017 Nov 9:12:8171-8183. [Abstract]
PC12 cell fluorescence images of baseline (before ATP stimulation), 0 s (the brightest fluorescence images after ATP stimulation), 50 s, 100 s, 150 s, and 200 s. Ca2+ peak increase (∆F/F0) in PC12 cells incubated with A-317491 salt, CSOSA/NLC, and CSOSA/NLC/A-317491 for predetermined time under 100 μM ATP stimulation.
-
Exp Physiol
Amplified P2X3 pathway activity in muscle afferent dorsal root ganglion neurons and exercise pressor reflex regulation in hindlimb ischaemia-reperfusion. [Abstract]2024 Apr;109(4):524-534. PMID: 38213082 -
Biochem Biophys Res Commun
Inflammatory mediator bradykinin increases population of sensory neurons expressing functional T-type Ca(2+) channels. [Abstract]2016 Apr 29;473(2):396-402. PMID: 26944020 -
Neurourol Urodyn
Estrogen inhibits bladder overactivity in rats with cyclophosphamide-induced cystitis via downregulating the expression of P2X3 receptors in bladder epithelium cells. [Abstract]2022 Jan;41(1):174-187. PMID: 34622458
Solvent & Solubility
H2O : 100 mg/mL (164.86 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (82.43 mM); Clear solution; Need ultrasonic
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
[1]. Jarvis MF, et, al. 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 Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84. [Content Brief]
[2]. Wu G, et, al. A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.6486 mL | 8.2431 mL | 16.4861 mL | 41.2154 mL |
| 5 mM | 0.3297 mL | 1.6486 mL | 3.2972 mL | 8.2431 mL | |
| 10 mM | 0.1649 mL | 0.8243 mL | 1.6486 mL | 4.1215 mL | |
| 15 mM | 0.1099 mL | 0.5495 mL | 1.0991 mL | 2.7477 mL | |
| 20 mM | 0.0824 mL | 0.4122 mL | 0.8243 mL | 2.0608 mL | |
| 25 mM | 0.0659 mL | 0.3297 mL | 0.6594 mL | 1.6486 mL | |
| 30 mM | 0.0550 mL | 0.2748 mL | 0.5495 mL | 1.3738 mL | |
| 40 mM | 0.0412 mL | 0.2061 mL | 0.4122 mL | 1.0304 mL | |
| 50 mM | 0.0330 mL | 0.1649 mL | 0.3297 mL | 0.8243 mL | |
| 60 mM | 0.0275 mL | 0.1374 mL | 0.2748 mL | 0.6869 mL | |
| 80 mM | 0.0206 mL | 0.1030 mL | 0.2061 mL | 0.5152 mL | |
| 100 mM | 0.0165 mL | 0.0824 mL | 0.1649 mL | 0.4122 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
A-317491 sodium salt hydrate Related Classifications
HY-15568A Related Classifications
Powered by Bioz