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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
Purity: 99.51%
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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Purity:99.51%
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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] |
| Synonyms | 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/Shipping at ambient temperature. | |||||||||||||||
| Solubility Information | DMSO: 4 mg/mL (7.33 mM), when pH is adjusted to 5~6 with HCl. Sonication is recommmended. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (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.
(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 μLSaline/PBS/ddH2O 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 μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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