Camlipixant
Based on 1 Customer Validation
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.76%
- CAS 番号: 1621164-74-6
- 分子式: C23H24F2N4O4
- 分子量:458.46
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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P2X Receptor アイソフォーム固有の製品をすべて表示
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生物活性
IC50: 25 nM (hP2X3), >24000 nM (hP2X2/3), 92 nM (rP2X3), 1820 nM (rP2X2/3), 126 nM (gpP2X3), 3450 nM (gpP2X2/3)[1]
Camlipixant (BLU-5937; 500 nM) blocks ATP-mediated dorsal root ganglion (DRG) neuron sensitization[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Camlipixant (BLU-5937; 10-20 mg/kg; i.p.) does not alter taste perception as compared to control animals[1].
Camlipixant (BLU-5937) exhibits excellent drug-like characteristics, including good oral bioavailability, low predicted clearance in human, no blood-brain barrier permeability and high safety margin versus human predicted efficacious exposure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Dunkin Hartley guinea pigs[1]
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Dosage:0.3, 3, 30 mg/kg
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Administration:PO, approximately 2 h prior to tussive agent exposure
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Result:Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs. Reduced significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1621164-74-6
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性状 Solid
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分子量 458.46
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分子式 C23H24F2N4O4
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Color White to off-white
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SMILES
O=C(N1C[C@H](CC2=C(C3=C(F)C=C(C(NC)=O)C=C3F)N=C4C=C(C)C=CN42)OCC1)OC
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別名
BLU-5937
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (218.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMSO : 100 mg/mL (218.12 mM; ultrasonic and adjust pH to 3 with 1M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / DMSO | 1 mM | 2.1812 mL | 10.9061 mL | 21.8122 mL | 54.5304 mL |
| 5 mM | 0.4362 mL | 2.1812 mL | 4.3624 mL | 10.9061 mL | |
| 10 mM | 0.2181 mL | 1.0906 mL | 2.1812 mL | 5.4530 mL | |
| 15 mM | 0.1454 mL | 0.7271 mL | 1.4541 mL | 3.6354 mL | |
| 20 mM | 0.1091 mL | 0.5453 mL | 1.0906 mL | 2.7265 mL | |
| 25 mM | 0.0872 mL | 0.4362 mL | 0.8725 mL | 2.1812 mL | |
| 30 mM | 0.0727 mL | 0.3635 mL | 0.7271 mL | 1.8177 mL | |
| 40 mM | 0.0545 mL | 0.2727 mL | 0.5453 mL | 1.3633 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0906 mL | |
| 60 mM | 0.0364 mL | 0.1818 mL | 0.3635 mL | 0.9088 mL | |
| 80 mM | 0.0273 mL | 0.1363 mL | 0.2727 mL | 0.6816 mL | |
| 100 mM | 0.0218 mL | 0.1091 mL | 0.2181 mL | 0.5453 mL |
Camlipixant 関連分類
HY-136026 関連分類
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