A-317491sodiumsalthydrate
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 606.57 |
| Molecular Formula | C33H29NNaO9 |
| 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 |
3 Publications Citing Use of MCE
Summary
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X 3 and P2X 2/3 receptors , with K i s of 22, 22, 9, and 92 nM for hP2X 3 , rP2X 3 , hP2X 2/3 , and rP2X 2/3 , 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 P2X 3 and P2X 2/3 receptor-mediated calcium flux [1] [2] .
IC50 & Target
Ki: 22 nM (hP2X3), 22 nM (rP2X3), 9 nM (hP2X2/3), 92 nM (rP2X2/3) [1]
In Vitro
A-317491 potently blocks recombinant human and rat P2X
3
and P2X
2/3
receptor-mediated calcium flux (K
i
=22-92 nM)
[1]
.
A-317491 (1 nM-10 μM) produces a concentration-dependent block of dorsal root ganglion (DRG) currents with an IC
50
of 15 nM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
A-317491 (0.1-30 mg/kg; a single s.c.) dose-dependently reverses inflammatory mechanical hyperalgesia in rats
[2]
.
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]
.
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. |
Appearance
Solid
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)
Solvent & Solubility
H 2 O : 100 mg/mL ( 164.86 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6486 mL | 8.2431 mL | 16.4861 mL |
| 5 mM | 0.3297 mL | 1.6486 mL | 3.2972 mL |
| 10 mM | 0.1649 mL | 0.8243 mL | 1.6486 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (82.43 mM); Clear solution; Need ultrasonic
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.
- [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.