| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
IC50: 8 nM (P2X3 receptor)[1]
Eliapixant targets the P2X3 purinoreceptor, a ligand-gated ion channel activated by ATP. It acts as a selective antagonist, blocking ATP-mediated activation of sensory neurons. By inhibiting P2X3 signaling, Eliapixant reduces neuronal sensitization and may alleviate chronic cough, overactive bladder, and pain. |
|---|---|
| ln Vitro |
In vitro, Eliapixant is a potent and selective P2X3 receptor antagonist with an IC50 of 8 nM. It selectively inhibits P2X3 over other purinergic receptors. The compound effectively blocks ATP-induced calcium influx in cells expressing P2X3 receptors.
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| ln Vivo |
Eliapixant has applications in the research of cough and diabetic problems [1].
In vivo activity data for Eliapixant are not extensively detailed in the available sources. The compound is orally bioavailable and is being investigated for the treatment of refractory chronic cough. Specific in vivo efficacy data are not provided. |
| Enzyme Assay |
The in vitro receptor binding assay for Eliapixant involves measuring its affinity for the P2X3 receptor. Radioligand binding assays or fluorescence-based calcium influx assays are performed using cells expressing the P2X3 receptor. The IC50 is determined by measuring the inhibition of ATP-induced calcium influx.
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| Cell Assay |
Cellular assays are performed using cell lines expressing the P2X3 receptor. Cells are loaded with a calcium-sensitive fluorescent dye and treated with Eliapixant at various concentrations. ATP is then added to stimulate the receptor, and calcium influx is measured. The compound's antagonist activity is determined by its ability to block the calcium response.
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| Animal Protocol |
In vivo animal studies for Eliapixant are not detailed in the available sources. The compound is orally bioavailable. Specific animal models and dosing regimens are not described.
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| ADME/Pharmacokinetics |
Eliapixant is an orally bioavailable compound. This property is favorable for in vivo studies and potential therapeutic applications. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for Eliapixant are not reported in the available sources. As an investigational compound, it is used for research purposes only.
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| References |
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| Additional Infomation |
Eliapixant is an orally bioavailable purinergic receptor P2X ligand-gated ion channel 3 (P2RX3) antagonist that may be used to suppress pain and chronic cough. After oral administration, eliapixant selectively binds to and inhibits P2RX3 expressed on sensory nerve fibers. This may inhibit P2RX3-mediated afferent nerve fiber signaling, including respiratory afferent nerve fiber signaling, thereby suppressing pain and chronic cough. P2RX3 plays an important role in the cough reflex and is also a natural mediator of pain and neurogenic inflammation.
Indications Treatment of unexplained or chronic refractory cough Eliapixant is a research compound being investigated for the treatment of refractory chronic cough, overactive bladder, and pain. It is a potent and selective P2X3 receptor antagonist. The compound is available from chemical suppliers for research use only. |
| Molecular Formula |
C22H21F3N4O3S
|
|---|---|
| Molecular Weight |
478.4874
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| Exact Mass |
478.13
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| Elemental Analysis |
C, 55.22; H, 4.42; F, 11.91; N, 11.71; O, 10.03; S, 6.70
|
| CAS # |
1948229-21-7
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| PubChem CID |
121397587
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| Appearance |
White to off-white solid powder
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| Density |
1.360±0.06 g/cm3(Predicted)
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
665
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
S1C(C([H])([H])[H])=C([H])N=C1C1=C([H])C(C(N([H])[C@]([H])(C([H])([H])[H])C2=C([H])N=C(C(F)(F)F)N=C2[H])=O)=C([H])C(=C1[H])O[C@@]1([H])C([H])([H])OC([H])([H])C1([H])[H]
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| InChi Key |
GTQPEQGDLVSFJO-CXAGYDPISA-N
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| InChi Code |
InChI=1S/C22H21F3N4O3S/c1-12-8-26-20(33-12)15-5-14(6-18(7-15)32-17-3-4-31-11-17)19(30)29-13(2)16-9-27-21(28-10-16)22(23,24)25/h5-10,13,17H,3-4,11H2,1-2H3,(H,29,30)/t13-,17-/m1/s1
|
| Chemical Name |
3-(5-methyl-1,3-thiazol-2-yl)-5-[(3R)-oxolan-3-yl]oxy-N-[(1R)-1-[2-(trifluoromethyl)pyrimidin-5-yl]ethyl]benzamide
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| Synonyms |
Eliapixant; BAY 1817080; BAY-1817080; BAY1817080;
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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 : ~33.33 mg/mL (~69.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0899 mL | 10.4495 mL | 20.8991 mL | |
| 5 mM | 0.4180 mL | 2.0899 mL | 4.1798 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0899 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.
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