BVT 2733
Based on 4 publication(s) in Google Scholar
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.
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- Pureza: 99.24%
- No. CAS: 376640-41-4
- Fòrmula: C17H21ClN4O3S2
- Peso molecular:428.96
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) BVT 2733
More
Actividad biológica
IC50: 96 nM (mouse 11β-HSD1)IC50: 3341 nM (human 11β-HSD1)[1]
BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 μM) reduces MCP-1 expression in fully differentiation adipocytes[3].BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium?in J774.1 macrophages by Elisa[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Differentiation adipocytes
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Concentration:100 μM
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Incubation Time:24 hours
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Result:Down-regulated MCP-1 mRNA level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Collagen-induced arthritis (CIA) mice[2]
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Dosage:100 mg/kg
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Administration:Oral administration; twice daily; 2 weeks
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Result:Reduced synovial inflammation and joint destruction.
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Animal Model:C57BL/6J mice[3]
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Dosage:100 mg/kg
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Administration:Oral administration; dosed (09.00 and 17.00 h); last 4 weeks
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Result:Improved metabolic homeostasis and suppressed the inflammation of adipose tissue in diet-induced obese mice.
Chemical Information
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No. CAS 376640-41-4
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Appearance Solid
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Peso molecular 428.96
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Fòrmula C17H21ClN4O3S2
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Color Off-white to pink
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SMILES
ClC1=C(C)C(S(NC2=NC(CC(N3CCN(C)CC3)=O)=CS2)(=O)=O)=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
2022 May;12(5):2358-2373. PMID: 35646525 -
Int J Biol Sci
The GR-gp78 Pathway is involved in Hepatic Lipid Accumulation Induced by Overexpression of 11β-HSD1. [Abstract]2022 Apr 30;18(8):3107-3121. PMID: 35637957 -
J Ethnopharmacol
Glycyrrhizic acid and patchouli alcohol in Huoxiang Zhengqi attenuate intestinal inflammation and barrier injury via regulating endogenous corticosterone metabolism mediated by 11β-HSD1. [Abstract]2024 Nov 1:119025. PMID: 39489360 -
Mol Med Rep
11β‑hydroxysteroid dehydrogenase‑1 is associated with the activation of hepatic stellate cells in the development of hepatic fibrosis. [Abstract]2020 Oct;22(4):3191-3200. PMID: 32945429
Solvente y solubilidad
DMSO : 50 mg/mL (116.56 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.83 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 (5.83 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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. 11β-hydroxydehydrogenase 1 (11β-HSD1) Inhibitor in Development
[2]. Zhang L, et al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis. Int Immunopharmacol. 2013 Nov;17(3):489-94. [Content Brief]
[3]. Wang L, et al. BVT.2733, a selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, attenuates obesity and inflammation in diet-induced obese mice. PLoS One. 2012;7(7):e40056. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3312 mL | 11.6561 mL | 23.3122 mL | 58.2805 mL |
| 5 mM | 0.4662 mL | 2.3312 mL | 4.6624 mL | 11.6561 mL | |
| 10 mM | 0.2331 mL | 1.1656 mL | 2.3312 mL | 5.8280 mL | |
| 15 mM | 0.1554 mL | 0.7771 mL | 1.5541 mL | 3.8854 mL | |
| 20 mM | 0.1166 mL | 0.5828 mL | 1.1656 mL | 2.9140 mL | |
| 25 mM | 0.0932 mL | 0.4662 mL | 0.9325 mL | 2.3312 mL | |
| 30 mM | 0.0777 mL | 0.3885 mL | 0.7771 mL | 1.9427 mL | |
| 40 mM | 0.0583 mL | 0.2914 mL | 0.5828 mL | 1.4570 mL | |
| 50 mM | 0.0466 mL | 0.2331 mL | 0.4662 mL | 1.1656 mL | |
| 60 mM | 0.0389 mL | 0.1943 mL | 0.3885 mL | 0.9713 mL | |
| 80 mM | 0.0291 mL | 0.1457 mL | 0.2914 mL | 0.7285 mL | |
| 100 mM | 0.0233 mL | 0.1166 mL | 0.2331 mL | 0.5828 mL |
BVT 2733 Related Classifications
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