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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
BVT-2733 is a selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, which attenuates obesity and inflammation in diet-induced obese mice. BVT-2733 protects osteoblasts against endogenous glucocorticoid induced dysfunction. BVT-2733 exhibits an anti-inflammatory effect on CIA. This protective effect is, at least partly, mediated by inhibition of the NF-κB and NLRP1 inflammasome signaling pathways. 11β-Hydroxysteroid dehydrogenase 1 (11β-HSD1) plays an important role in inflammation. 11β-HSD1 inhibition may represent a potential therapeutic target for RA patients.
| ln Vitro |
In fully developed adipocytes, co-treatment of BVT 2733 (100 μM; 24 hours) with PA (100 μM) decreases MCP-1 expression [3]. Elisa examined the levels of inflammatory proteins (MCP-1, IL-6) in the J774.1 macrophage culture media and found that BVT 2733 (50-100 μM; 24 hours) reduced them [3].
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| ln Vivo |
Oral BVT-2733 (100 mg/kg; twice daily; 2 weeks) decreases anti-CII levels and the severity of arthritis in CIA mice as well as the levels of TNF-α, IL-1β, IL-6, and IL-17 in their serum[2]. In comparison to control mice, BVT 2733 (oral; 100 mg/kg; dosage [09:00 and 17:00 hours); last 4 weeks) showed decreased body weight and improved insulin sensitivity and glucose tolerance. Moreover, it suppresses the expression of genes linked to inflammation, such as tumor necrosis factor alpha (TNF-α), monocyte chemoattractant protein 1 (MCP-1), and the quantity of macrophages that enter the body's adipose tissue [3].
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| Cell Assay |
RT-PCR[3]
Cell Types: Differentiated Adipocytes Tested Concentrations: 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Downregulation of MCP-1 mRNA levels. |
| Animal Protocol |
Animal/Disease Models: Collagen-induced arthritis (CIA) mice [2]
Doses: 100 mg/kg Route of Administration: Oral; twice (two times) daily; 2 weeks Experimental Results: diminished synovial inflammation and joint destruction. Animal/Disease Models: C57BL/6J mice [3] Doses: 100 mg/kg Route of Administration: po (po (oral gavage)) Take the drug (09:00 and 17:00); Results in the past 4 weeks: Improved metabolic homeostasis in diet-induced obese mice and inhibits inflammation of adipose tissue. |
| References |
[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. [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. |
| Molecular Formula |
C17H21CLN4O3S2
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|---|---|
| Molecular Weight |
428.95
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| Exact Mass |
428.07436
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| CAS # |
376640-41-4
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| Related CAS # |
376640-41-4
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| SMILES |
CN1CCN(C(CC2=CSC(NS(=O)(C3=CC=CC(Cl)=C3C)=O)=N2)=O)CC1
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| InChi Key |
YDPRNGAPPNPYQQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21ClN4O3S2/c1-12-14(18)4-3-5-15(12)27(24,25)20-17-19-13(11-26-17)10-16(23)22-8-6-21(2)7-9-22/h3-5,11H,6-10H2,1-2H3,(H,19,20)
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| Chemical Name |
3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide
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| Synonyms |
BVT-2733 BVT 2733 BVT2733 BVT.2733
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~50 mg/mL (~116.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 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 (5.83 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 (5.83 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 | 2.3313 mL | 11.6564 mL | 23.3127 mL | |
| 5 mM | 0.4663 mL | 2.3313 mL | 4.6625 mL | |
| 10 mM | 0.2331 mL | 1.1656 mL | 2.3313 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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