TRPV2-selective blocker 1
Based on 2 publication(s) in Google Scholar
TRPV2-selective blocker 1 is a TRPV2-selective blocker that inhibits calcium influx and ionic currents. TRPV2-selective blocker 1 exhibits an IC50 of 6.3 μM against rat TRPV2, and shows no activity against TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 attenuates macrophage phagocytosis, LPS-induced macrophage migration, and calcium microdomains generated by peripheral TRPV2. TRPV2-selective blocker 1 is non-cytotoxic and can be used to investigate the function of TRPV2 during immune processes.
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- 純度: 99.84%
- CAS 番号: 2242724-49-6
- 分子式: C15H18OS2
- 分子量:278.43
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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
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MedChemExpress（MCE）の使用を引用している文献 TRPV2-selective blocker 1
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生物活性
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TRPV2 6.3 μM (IC50) |
TRPV2-selective blocker 1 (0.1-100 μM; 30 min, 60-second) potently and selectively inhibits rat TRPV2-mediated Ca2+ influx in HEK_TRPV2 cells with an IC50 of 6.3 μM, with no activity on TRPV1, TRPV3, or TRPV4 channels at concentrations up to 50 μM[1].
TRPV2-selective blocker 1 (20 μM; 30 min) completely blocks TRPV2-mediated [Ca2+]i increases in HEK_TRPV2 cells activated by either high-dose 2-APB or a low-dose 2-APB (HY-W009724)/Probenecid (HY-B0545) combination[1].
TRPV2-selective blocker 1 (0.1-20 μM) inhibits rat TRPV2 ionic currents in HEK_TRPV2 cells with an IC50 of 0.8 μM, and reduces single-channel open probability in a membrane-delimited manner[1].
TRPV2-selective blocker 1 (20 μM; 30 min) strongly reduces TRPV2-mediated [Ca2+]i increases in primary mouse BMDM activated by 300 μM 2-APB[1].
TRPV2-selective blocker 1 (20-50 μM; 1 h, 24 h) attenuates phagocytosis of zymosan and S. aureus bioparticles in primary mouse BMDM, with no cytotoxicity at concentrations up to 50 μM after 24 h incubation[1].
TRPV2-selective blocker 1 (20 μM; 1-2 h, 14 h) attenuates LPS-induced migration of primary mouse BMDM and blocks the enhanced migration caused by TRPV2 activation with a 2-APB/probenecid combination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2242724-49-6
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性状 Solid
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分子量 278.43
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分子式 C15H18OS2
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Color White to off-white
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SMILES
CC(CC(C)/C(C1=CC=CC=C1)=C2SCCS\2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 100 mg/mL (359.16 mM; Need ultrasonic; 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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: ≥ 0.83 mg/mL (2.98 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (2.98 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
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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 (protect from light, stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5916 mL | 17.9578 mL | 35.9157 mL | 89.7892 mL |
| 5 mM | 0.7183 mL | 3.5916 mL | 7.1831 mL | 17.9578 mL | |
| 10 mM | 0.3592 mL | 1.7958 mL | 3.5916 mL | 8.9789 mL | |
| 15 mM | 0.2394 mL | 1.1972 mL | 2.3944 mL | 5.9859 mL | |
| 20 mM | 0.1796 mL | 0.8979 mL | 1.7958 mL | 4.4895 mL | |
| 25 mM | 0.1437 mL | 0.7183 mL | 1.4366 mL | 3.5916 mL | |
| 30 mM | 0.1197 mL | 0.5986 mL | 1.1972 mL | 2.9930 mL | |
| 40 mM | 0.0898 mL | 0.4489 mL | 0.8979 mL | 2.2447 mL | |
| 50 mM | 0.0718 mL | 0.3592 mL | 0.7183 mL | 1.7958 mL | |
| 60 mM | 0.0599 mL | 0.2993 mL | 0.5986 mL | 1.4965 mL | |
| 80 mM | 0.0449 mL | 0.2245 mL | 0.4489 mL | 1.1224 mL | |
| 100 mM | 0.0359 mL | 0.1796 mL | 0.3592 mL | 0.8979 mL |
TRPV2-selective blocker 1 関連分類
HY-157131 関連分類
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