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Gefapixant citrate
🥰Excellent
Catalog No. T63846Cas No. 2310299-91-1
Alias RO4926219 citrate, RO 4926219 citrate, MK-7264 citrate, MK7264 citrate, AF-219 citrate, AF219 citrate
Gefapixant citrate (AF-219 citrate) is an orally available, highly potent P2X3 receptor antagonist with antitussive properties that inhibits hP2X2/3. It can be used to study chronic cough.
Gefapixant citrate
🥰Excellent
Catalog No. T63846Alias RO4926219 citrate, RO 4926219 citrate, MK-7264 citrate, MK7264 citrate, AF-219 citrate, AF219 citrateCas No. 2310299-91-1
Gefapixant citrate (AF-219 citrate) is an orally available, highly potent P2X3 receptor antagonist with antitussive properties that inhibits hP2X2/3. It can be used to study chronic cough.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $58 | In Stock | |
| 50 mg | $238 | In Stock | |
| 100 mg | $428 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| Description | Gefapixant citrate (AF-219 citrate) is an orally available, highly potent P2X3 receptor antagonist with antitussive properties that inhibits hP2X2/3. It can be used to study chronic cough. |
| In vitro | Gefapixant citrate did not inhibit any receptor that did not contain a P2X3 subunit, and its IC50 values exceeded 10,000 nM on recombinant hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7 channels. [1] |
| In vivo | In a rat model of knee osteoarthritis, Gefapixant citrate (administered orally twice daily for 7 days) was able to attenuate the abnormal response on the weight-loading side and completely reversed the significant nociceptive hypersensitivity at the two higher doses (20 mg/kg and 60 mg/kg) (the model was established by intra-articular injections of monoiodoacetic acid and was observed for 14 days post-injection). [2] |
| Alias | RO4926219 citrate, RO 4926219 citrate, MK-7264 citrate, MK7264 citrate, AF-219 citrate, AF219 citrate |
| Molecular Weight | 545.52 |
| Formula | C20H27N5O11S |
| Cas No. | 2310299-91-1 |
| Smiles | O=C(O)CC(O)(C(=O)O)CC(=O)O.O=S(=O)(N)C=1C=C(OC2=CN=C(N=C2N)N)C(=CC1OC)C(C)C |
Storage & Solubility Information
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
| Solubility Information | DMSO: 4 mg/mL (7.33 mM), Adjust pH to 5-6 with HCl and sonication is recommended. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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