| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
P2X3 antagonist 34 (BLU-5937; 500 nM) antagonizes P2X3 homotrimeric receptors to prevent αβ-meATP-induced sensitization of isolated primary nociceptors in the rat dorsal root ganglion (DRG). as well as the discharge process. Following washout, both the sensitizing effect of αβ-meATP and the inhibitory impact of P2X3 antagonist 34 are reversible [1].
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| ln Vivo |
The administration of P2X3 antagonist 34 (BLU-5937; 0.3-0 mg/kg, oral; male Dunkin Hartley guinea pigs) to guinea pigs resulted in a dose-dependent reduction in the number of coughs induced by citric acid, which was caused by histamine. model [1]. It has also been demonstrated that the P2X3 antagonist 34 (BLU-5937; orally administered at 3 and 30 mg/kg) significantly and dose-dependently reduces the ATP-induced potentiation of citric acid-induced cough in guinea pigs [1].
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| Animal Protocol |
Animal/Disease Models: Male Dunkin Hartley guinea pig [1]
Doses: 0.3 mg/kg, 3 mg/kg, 30 mg/kg Route of Administration: Oral Experimental Results: Significant reduction in the number of histamine-induced citric acid-induced coughs in a dose-dependent manner Way. |
| References |
| Molecular Formula |
C24H26F2N4O3
|
|---|---|
| Molecular Weight |
456.4851
|
| Exact Mass |
456.197
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| CAS # |
2417288-67-4
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| PubChem CID |
132129813
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
701
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C([H])=C(C(N([H])C([H])([H])[H])=O)C([H])=C(C=1C1=C(C([H])([H])[C@@]2([H])C([H])([H])N(C(=O)OC([H])([H])[H])C([H])([H])C([H])([H])C2([H])[H])N2C([H])=C([H])C(C([H])([H])[H])=C([H])C2=N1)F
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| InChi Key |
HHJIZLMOCIYWJF-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C24H26F2N4O3/c1-14-6-8-30-19(10-15-5-4-7-29(13-15)24(32)33-3)22(28-20(30)9-14)21-17(25)11-16(12-18(21)26)23(31)27-2/h6,8-9,11-12,15H,4-5,7,10,13H2,1-3H3,(H,27,31)/t15-/m0/s1
|
| Chemical Name |
methyl (3S)-3-[[2-[2,6-difluoro-4-(methylcarbamoyl)phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]piperidine-1-carboxylate
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| Synonyms |
P2X3 antagonist 34; P2X3 antagonist 34
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~219.06 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 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: ≥ 2.5 mg/mL (5.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 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: ≥ 2.5 mg/mL (5.48 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 | 2.1906 mL | 10.9531 mL | 21.9063 mL | |
| 5 mM | 0.4381 mL | 2.1906 mL | 4.3813 mL | |
| 10 mM | 0.2191 mL | 1.0953 mL | 2.1906 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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