| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
BVT-2733 targets 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), a key enzyme that converts inactive cortisone to active cortisol. By inhibiting 11β-HSD1, the compound reduces local cortisol production in tissues such as liver and adipose tissue. This modulation of glucocorticoid metabolism has therapeutic potential for metabolic disorders including obesity, insulin resistance, and type 2 diabetes, as well as inflammatory conditions such as arthritis.
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| 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].
In vitro, BVT-2733 is a potent and selective inhibitor of 11β-HSD1 with an IC50 of 96 nM against the mouse enzyme. It has a Ki of 1 μM for mouse 11β-HSD1. The compound is a non-steroidal small molecule that shows selectivity for 11β-HSD1 over other related enzymes. Its activity is assessed using enzyme inhibition assays with recombinant 11β-HSD1. |
| 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].
In vivo, BVT-2733 is orally active and has been studied in preclinical models of metabolic disorders such as obesity and insulin resistance. By inhibiting 11β-HSD1, the compound reduces local cortisol production, which may improve insulin sensitivity, reduce hepatic glucose production, and attenuate inflammatory responses. The compound has also been studied in inflammatory conditions such as arthritis. |
| Enzyme Assay |
In vitro enzyme assays for BVT-2733 measure its inhibition of 11β-HSD1 activity. The enzyme is incubated with its substrate (cortisone) and cofactor (NADPH) in the presence of varying concentrations of the compound. The conversion of cortisone to cortisol is quantified by HPLC or immunoassay. The IC50 of 96 nM against mouse 11β-HSD1 is determined from dose-response curves. The Ki of 1 μM is calculated from enzyme kinetics.
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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. In vitro cell-based assays for BVT-2733 use cells expressing 11β-HSD1, such as hepatocytes or adipocytes. Cells are treated with serial dilutions of the compound, and 11β-HSD1 activity is measured by assessing the conversion of cortisone to cortisol. Cellular cortisol levels are quantified by ELISA or LC-MS/MS. The compound's effects on cell viability and metabolic endpoints are assessed in parallel. |
| 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. In vivo animal models for BVT-2733 include mouse and rat models of obesity, insulin resistance, and type 2 diabetes. The compound is administered orally, and its effects on body weight, glucose tolerance, insulin sensitivity, and inflammatory markers are evaluated. Models of inflammatory conditions such as arthritis are also used to assess anti-inflammatory efficacy. Pharmacodynamic studies measure 11β-HSD1 inhibition in target tissues. |
| ADME/Pharmacokinetics |
BVT-2733 has a molecular formula of C17H21ClN4O3S2 and a molecular weight of 428.96. The compound is orally bioavailable and is administered orally in preclinical studies. It is soluble in DMSO and other organic solvents. The compound is stored as a powder at -20°C. Pharmacokinetic parameters including half-life, bioavailability, and tissue distribution are documented in research publications.
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| Toxicity/Toxicokinetics |
The toxicity profile of BVT-2733 is characterized in preclinical safety studies. As an 11β-HSD1 inhibitor, the compound is generally well-tolerated at therapeutic doses. Common adverse effects may include gastrointestinal discomfort. The compound is for research use only and not for human use. Appropriate safety precautions should be taken during handling. The safety margin is determined from toxicology studies.
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| References | |
| Additional Infomation |
BVT-2733 is a non-steroidal small molecule that acts as a selective 11β-HSD1 inhibitor. It is also known as BVT 2733 and BVT2733. The compound is potently active against the mouse enzyme with an IC50 of 96 nM and has a Ki of 1 μM. BVT-2733 is used in preclinical research targeting metabolic disorders (obesity, insulin resistance) and inflammatory conditions (arthritis). It is used for research purposes only and is not approved for clinical use.
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| Molecular Formula |
C17H21CLN4O3S2
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| Molecular Weight |
428.95
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| Exact Mass |
428.074
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| CAS # |
376640-41-4
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| Related CAS # |
376640-41-4
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| PubChem CID |
6918651
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| Appearance |
Off-white to pink solid powder
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| LogP |
3.251
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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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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| HS Tariff Code |
2934.99.9001
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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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