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Eliapixant (BAY-1817080) is a potent and selective antagonist of P2X3 purinoreceptor (IC50 = 8 nM) and may be used for treating refractory chronic cough.
| Targets |
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| ln Vivo |
Eliapixant has applications in the research of cough and diabetic problems [1].
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| References |
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| Additional Infomation |
Eliapixant is an orally bioavailable antagonist of the purinergic receptor P2X ligand-gated ion channel 3 (P2RX3), which may potentially be used to suppress pain and chronic cough. Upon 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 tract afferent nerve fiber signaling, and result in the suppression of pain and chronic cough. P2RX3 plays an important role in the cough reflex. It is also a natural mediator of pain and neurogenic inflammation.
Drug Indication Treatment of unexplained or chronic refractory cough |
| Molecular Formula |
C22H21F3N4O3S
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|---|---|
| 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
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| 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
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| 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
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| 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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