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Purity: ≥98%
Gefapixant (also known as AF-219 and MK-7264) is a novel, potent, and orally bioactive P2X3 receptor (P2X3R) antagonist with antitussive effects, and may be used for chronic cough. It inhibits P2X3R with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Treating pain by inhibiting ATP activation of P2X3-containing receptors heralds an exciting new approach to pain management, and Afferent's program marks the vanguard in a new class of drugs poised to explore this approach to meet the significant unmet needs in pain management. P2X3 receptor subunits are expressed predominately and selectively in so-called C- and Aδ-fiber primary afferent neurons in most tissues and organ systems, including skin, joints, and hollow organs, suggesting a high degree of specificity to the pain sensing system in the human body. P2X3 antagonists block the activation of these fibers by ATP and stand to offer an alternative approach to the management of pain and discomfort.
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| ln Vitro |
For recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7 channels, the IC50 values are greater than 10,000 nM, indicating that gefapixant has no inhibitory impact on any receptor that contains non-P2X3 subunits [1].
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| ln Vivo |
Within 14 days of intra-articular monoiodoacetate injection, gefapixant (7 days bid, oral) totally reversed overt hyperalgesia and decreased weight-bearing laterality at two higher doses in a rat model of knee osteoarthritis [2].
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| References |
[1]. Anthony P. Ford, et al. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267.
[2]. Ford AP, In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signal. 2012 Feb;8(Suppl 1):3-26. [3]. Martin Nguyen A, et al. Validation of a visual analog scale for assessing cough severity in patients with chronic cough. Ther Adv Respir Dis. 2021 Jan-Dec;15:17534666211049743 |
| Molecular Formula |
C14H19N5O4S
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|---|---|
| Molecular Weight |
353.39676117897
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| CAS # |
1015787-98-0
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| Related CAS # |
Gefapixant citrate;2310299-91-1
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| SMILES |
S(C1=CC(=C(C=C1OC)C(C)C)OC1=CN=C(N)N=C1N)(N)(=O)=O
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| 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)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~14.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% PBS (add these co-solvents sequentially from left to right, and one by one), clear solution.
Solubility in Formulation 2: ≥ 0.5 mg/mL (1.41 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 5.0 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. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.5 mg/mL (1.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8297 mL | 14.1483 mL | 28.2965 mL | |
| 5 mM | 0.5659 mL | 2.8297 mL | 5.6593 mL | |
| 10 mM | 0.2830 mL | 1.4148 mL | 2.8297 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.
 Nocifensive data showing the effect of a P2X3 antagonist in preclinical models of joint hyperalgesia.Purinergic Signal.2012 Feb;8(Suppl 1):3-26. |
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 Systemic P2X3 receptor antagonism with AF-353 attenuates bone cancer pain behaviour in rats.Purinergic Signal.2012 Feb;8(Suppl 1):3-26. |
Effects of P2X3 antagonists in preclinical models of urinary bladder reflexes.Purinergic Signal.2012 Feb;8(Suppl 1):3-26. |
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