SB 452533
Based on 1 Customer Validation
SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8.
For research use only. We do not sell to patients.
- Purity: 99.11%
- CAS No.: 459429-39-1
- Formula: C18H22BrN3O
- Molecular Weight:376.29
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
SB 452533 is potent as an antagonist at the cloned recombinant rat TRPV1 receptor in HEK293 cells with a pKb of 7.7 and a pIC50 of 7.0[1].
SB-452533 reduces phosphorylation of CAMKK2 and AMPK[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Skeletal muscle (C2C12) cells
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Concentration:0, 50, 100, 200, and 400 μM
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Incubation Time:30 minutes; followed by 200 μM Capsaicin treatment for another 30 min.
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Result:Significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice bearing pulmonary fibrosis model[3]
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Dosage:2.5 mg/kg
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Administration:Treatment received daily drug via subcutaneous injection for 21 days
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Result:The effect (reduced Bleomycin-induced pulmonary fibrosis) of Cap were abolished in the presence of SB-452533.
Chemical Information
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CAS No. 459429-39-1
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Appearance Solid
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Molecular Weight 376.29
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Formula C18H22BrN3O
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Color White to off-white
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SMILES
O=C(NCCN(CC)C1=CC=CC(C)=C1)NC2=CC=CC=C2Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (265.75 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.64 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 (6.64 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (758 KB)
- English - EN (758 KB)
- Français - FR (758 KB)
- Deutsch - DE (758 KB)
- Norwegian - NO (758 KB)
- Español - ES (758 KB)
- Swedish - SV (758 KB)
- Italian - IT (758 KB)
- Portuguese - PT (758 KB)
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Handling Instructions (2659 KB)
References
[1]. Harshad K Rami, et al. Discovery of small molecule antagonists of TRPV1. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4. [Content Brief]
[2]. Parisa Vahidi Ferdowsi, et al. TRPV1 Activation by Capsaicin Mediates Glucose Oxidation and ATP Production Independent of Insulin Signalling in Mouse Skeletal Muscle Cells. Cells. 2021 Jun 21;10(6):1560. [Content Brief]
[3]. Lin Ming Lu, et al. Effect of small dose capsaicin for treatment of pulmonary fibrosis in mice and its mechanism. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2020 May;36(3):216-222. [Content Brief]
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). 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 | 2.6575 mL | 13.2876 mL | 26.5752 mL | 66.4381 mL |
| 5 mM | 0.5315 mL | 2.6575 mL | 5.3150 mL | 13.2876 mL | |
| 10 mM | 0.2658 mL | 1.3288 mL | 2.6575 mL | 6.6438 mL | |
| 15 mM | 0.1772 mL | 0.8858 mL | 1.7717 mL | 4.4292 mL | |
| 20 mM | 0.1329 mL | 0.6644 mL | 1.3288 mL | 3.3219 mL | |
| 25 mM | 0.1063 mL | 0.5315 mL | 1.0630 mL | 2.6575 mL | |
| 30 mM | 0.0886 mL | 0.4429 mL | 0.8858 mL | 2.2146 mL | |
| 40 mM | 0.0664 mL | 0.3322 mL | 0.6644 mL | 1.6610 mL | |
| 50 mM | 0.0532 mL | 0.2658 mL | 0.5315 mL | 1.3288 mL | |
| 60 mM | 0.0443 mL | 0.2215 mL | 0.4429 mL | 1.1073 mL | |
| 80 mM | 0.0332 mL | 0.1661 mL | 0.3322 mL | 0.8305 mL | |
| 100 mM | 0.0266 mL | 0.1329 mL | 0.2658 mL | 0.6644 mL |
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