Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
50mg |
|
||
Other Sizes |
|
Targets |
P2X3 Receptor
|
---|---|
ln Vitro |
Recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flow (Ki=22-92 nM) is potently blocked by A-317491 [1]. A concentration-dependent inhibition of dorsal root ganglion (DRG) currents is produced by A-317491 (1 nM-10 μM) with an IC50 of 15 nM[1].
|
ln Vivo |
A-317491 (0.1-30 mg/kg; one single SC) reverses inflammatory mechanical hyperalgesia in rats in a dose-dependent manner[2]. Plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg) are demonstrated by A-317491 (3-30 mg/kg; a single.v.)[2].
|
Animal Protocol |
Animal/Disease Models: Male adult SD (Sprague-Dawley) rats received an intraplantar injection of Freund's complete adjuvant[2] ]
Doses: 0.1, 1, 3, 10, 30 mg/kg Route of Administration: A single sc Experimental Results: Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration. |
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. |
Molecular Formula |
C33H29NNAO9
|
---|---|
Molecular Weight |
606.57
|
Related CAS # |
A-317491;475205-49-3
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
H2O :~100 mg/mL (~164.86 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (82.43 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.