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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $58 | In Stock | In Stock | |
| 50 mg | $238 | In Stock | In Stock | |
| 100 mg | $428 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.51%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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 | 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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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
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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