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Gefapixant
🥰Excellent
Catalog No. T5099Cas No. 1015787-98-0
Alias RO 4926219, MK-7264, AF219
Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
Gefapixant
🥰Excellent
Purity: 99.72%
Catalog No. T5099Alias RO 4926219, MK-7264, AF219Cas No. 1015787-98-0
Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $32 | In Stock | |
| 5 mg | $53 | In Stock | |
| 10 mg | $77 | In Stock | |
| 25 mg | $158 | In Stock | |
| 50 mg | $255 | In Stock | |
| 100 mg | $377 | In Stock | |
| 200 mg | $536 | In Stock |
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Purity:99.72%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. |
| Targets&IC50 | Recombinant hP2X3 homotrimers:~30 nM, P2X2/3 heterotrimeric receptors (human):100-250 nM |
| In vitro | The IC50 of Gefapixant has been reported as ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors, potencies very similar to those reported for recombinant rat receptors, and it displays no inhibitory impact on any non-P2X3 subunit-containing receptors (IC50 values>>10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7 channels). |
| In vivo | In a rat model for knee osteoarthritis (developed 14 days after the intra-articular injection of monoiodoacetate), oral administration of Gefapixant twice daily for seven days resulted in a significant attenuation of weight bearing asymmetry, with a full reversal of observable hyperalgesia at the two higher doses [2]. |
| Animal Research | A rodent model often employs for assessing the potential for drug effect in osteoarthritis (OA) pain is based on the intraarticular injection of monoiodoacetate (mIOA) into one knee joint of the rat. To measure the effect of Gefapixant on the weight bearing laterality and apparent hyperalgesia, Gefapixant is given by intraplantar or oral administration to the rats, with different concentrations (6, 20, and 60 mg/kg) two times a day and continues up to a week[2]. |
| Alias | RO 4926219, MK-7264, AF219 |
| Molecular Weight | 353.4 |
| Formula | C14H19N5O4S |
| Cas No. | 1015787-98-0 |
| Smiles | COc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1S(N)(=O)=O |
| Relative Density. | 1.391 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO: < 1 mg/mL (insoluble）  H2O: Insoluble |
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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% 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 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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