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25mg |
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50mg |
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Purity: ≥98%
A-317491 sodium, the tri-sodium salt of A-317491, which is a selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which inhibits calcium flux mediated by the receptors. The purinergic P2X3 and P2X2/3 receptors are in the peripheral nervous system almost exclusively confined to afferent sensory neurons, where they are found both at peripheral and central synapses. The P2X3 receptor is implicated in both neuropathic and inflammatory pain. It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management.
ln Vitro |
Recombinant human and rat P2X3 and P2X2/3 receptors (Ki=22-92 nM) efficiently block calcium flux[1]. The 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].
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ln Vivo |
In rats, inflammatory mechanical hyperalgesia is dose-dependently reversed by A-317491 (0.1–30 mg/kg; single subcutaneous injection) [2]. The plasma half-life of A-317491 (3–30 mg/kg; single subcutaneous injection) is 7.38 hours, while its clearance is 1.83 L/h/kg and its volume of distribution is 0.17 L/kg [2].
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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 |
C33H24NNA3O8
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Molecular Weight |
631.12
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CAS # |
475205-49-3
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Related CAS # |
A-317491 sodium salt hydrate
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(C1=C([H])C(C(=O)O[H])=C(C(=O)O[H])C([H])=C1C(=O)O[H])N(C([H])([H])C1C([H])=C([H])C([H])=C(C=1[H])OC1C([H])=C([H])C([H])=C([H])C=1[H])[C@]1([H])C2=C([H])C([H])=C([H])C([H])=C2C([H])([H])C([H])([H])C1([H])[H]
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.42 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5845 mL | 7.9224 mL | 15.8448 mL | |
5 mM | 0.3169 mL | 1.5845 mL | 3.1690 mL | |
10 mM | 0.1584 mL | 0.7922 mL | 1.5845 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.