| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
purinoreceptor[1]
Filapixant selectively targets the P2X3 homotrimeric receptor, a key mediator of the cough reflex. It is a purinergic receptor antagonist with high selectivity for P2X3 over P2X2/3 heterotrimers. This selectivity is important for minimizing off-target effects such as taste disturbance. The compound is orally active and primarily metabolized by CYP3A4, as demonstrated in in vitro metabolism studies. |
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| ln Vitro |
In vitro, filapixant potently antagonizes P2X3 receptor-mediated currents with high selectivity. When compared to other P2X3 antagonists such as gefapixant and eliapixant, filapixant exhibits substantially higher in vitro selectivity for P2X3 over P2X2/3. This improved selectivity is expected to translate into a better safety profile, particularly regarding taste alteration, which is mediated by P2X2/3 heterotrimers present on taste buds. Filapixant is primarily metabolized by CYP3A4 (0.1-1 microM).
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| ln Vivo |
In vivo, filapixant is effective in reducing cough in animal models of refractory chronic cough. As an orally active P2X3 antagonist, it has been investigated for its potential to treat chronic cough with a favorable selectivity profile that may avoid the taste-related side effects that have limited other P2X3 antagonists. Detailed in vivo efficacy data should be obtained from the primary literature.
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| Enzyme Assay |
For in vitro P2X3 antagonism assays, HEK293 cells expressing human P2X3 receptors are pre-incubated with filapixant (0.1-1000 nM) in assay buffer for 5-10 minutes. ATP (1-100 uM) is then applied to activate P2X3 receptors, and calcium influx is measured using a fluorescent calcium indicator (e.g., Fluo-4 AM). IC50 values are calculated using dose-response curve fitting. For selectivity, similar assays are performed on P2X2/3-expressing cells.
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| Cell Assay |
For cell-based assays, primary cultures of rat dorsal root ganglion (DRG) neurons or P2X3-expressing cell lines are treated with filapixant at concentrations ranging from 1-1000 nM for 30 minutes. Cells are then stimulated with ATP (10 uM), and P2X3-mediated calcium influx is measured. Supernatants can be analyzed for neuropeptide release (e.g., substance P, CGRP) by ELISA. Cell viability is assessed by MTT assay. The primary metabolic pathway involves CYP3A4 metabolism, which can be evaluated using human liver microsomes.
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| Animal Protocol |
For in vivo cough models, filapixant is typically formulated in an appropriate oral vehicle (e.g., 0.5% methylcellulose or PEG400) and administered orally by gavage to guinea pigs at doses ranging from 1-30 mg/kg, 1-2 hours prior to cough challenge. Cough is induced by inhalation of citric acid aerosol (0.4 M) for 5-10 minutes. The number of coughs is counted over the challenge period. Alternatively, histamine or ATP-induced cough hypersensitivity models can be used. Taste alteration is assessed using brief-access taste tests or two-bottle preference tests in rodents.
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| ADME/Pharmacokinetics |
Detailed PK data for filapixant are limited in publicly available sources. The compound is described as orally active, indicating good oral bioavailability. In vitro metabolism studies show that filapixant is primarily metabolized by CYP3A4. For species-specific PK parameters (Cmax, Tmax, t1/2, bioavailability, plasma protein binding), researchers should consult primary literature or conduct pilot PK studies in their model system.
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| Toxicity/Toxicokinetics |
Published toxicology data for filapixant are limited. Based on its high selectivity for P2X3 over P2X2/3 receptors, filapixant is expected to have a reduced risk of taste alteration compared to less selective P2X3 antagonists. In animal studies at therapeutic doses, no significant adverse events have been reported. Comprehensive toxicology studies have been conducted as part of preclinical development. Researchers should consult primary literature for specific safety data.
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| References | |
| Additional Infomation |
Filapixant is a small molecule drug. The international nonproprietary name stem "-pixant" in its name indicates that filapixant is a purinergic receptor (P2X) antagonist. The monoisotope molecular weight of filapixant is 521.17 Da.
Filapixant is in preclinical or early clinical development for refractory chronic cough. It is described as an active control for eliapixant (BAY1817080) in certain contexts. The compound was originally disclosed in patent WO2016091776A1. Filapixant is not approved for clinical use and is intended for research purposes only. It should be stored at -20degC, protected from moisture and light. |
| Molecular Formula |
C24H26F3N5O3S
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|---|---|
| Molecular Weight |
521.555154323578
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| Exact Mass |
521.17
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| CAS # |
1948232-63-0
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| PubChem CID |
121397607
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| Appearance |
White to light yellow solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
728
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S1C(C)=CN=C1C1C=C(C(N[C@H](C)C2=CN=C(C(F)(F)F)N=C2)=O)C=C(C=1)OC[C@H]1CN(C)CCO1
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| InChi Key |
MROBUJILSMBILX-FOIQADDNSA-N
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| InChi Code |
InChI=1S/C24H26F3N5O3S/c1-14-9-28-22(36-14)17-6-16(7-19(8-17)35-13-20-12-32(3)4-5-34-20)21(33)31-15(2)18-10-29-23(30-11-18)24(25,26)27/h6-11,15,20H,4-5,12-13H2,1-3H3,(H,31,33)/t15-,20-/m1/s1
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| Chemical Name |
3-[[(2R)-4-methylmorpholin-2-yl]methoxy]-5-(5-methyl-1,3-thiazol-2-yl)-N-[(1R)-1-[2-(trifluoromethyl)pyrimidin-5-yl]ethyl]benzamide
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| HS Tariff Code |
2934.99.9001
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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: 146.67 mg/mL (281.21 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5.5 mg/mL (10.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 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. Solubility in Formulation 2: 5.5 mg/mL (10.55 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5.5 mg/mL (10.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9173 mL | 9.5866 mL | 19.1732 mL | |
| 5 mM | 0.3835 mL | 1.9173 mL | 3.8346 mL | |
| 10 mM | 0.1917 mL | 0.9587 mL | 1.9173 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.
Link: https://clinicaltrials.gov/ct2/show/NCT03535168
Conditions:CoughLink: https://clinicaltrials.gov/ct2/show/NCT03789890
Conditions:Drug InteractionsLink: https://clinicaltrials.gov/ct2/show/NCT03212586
Conditions:Clinical Trials, Phase I as TopicProducts are for research use only; We do not sell to patients
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