BVT 2733 |
Catalog No.GC15738
One-Click Copy Product Info
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BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor with an IC50 value of 96nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 376640-41-4
Sample solution is provided at 25 µL, 10mM.
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BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor with an IC50 value of 96nM[1]. BVT 2733 inhibits the activity of the NF-κB/MAPK signaling pathway and prevents the activation of the NLRP3 inflammasome by targeting 11β-HSD1, thereby alleviating endothelial damage associated with sepsis[2]. BVT 2733 has been widely used in metabolic research to improve the liver function of diabetic mice[3].
In vitro, BVT 2733 pretreatment (100µM) for 1 hour inhibited the increase in mRNA expression levels of 11β-HSD1, IL-6, and IL-1β in lipopolysaccharide (LPS)-induced THP-1 cells, reduced ROS production, and maintained mitochondrial membrane potential homeostasis[4]. Treatment with 100µM BVT 2733 for 14 days protected MC3T3-E1 cells from the functional impairment induced by endogenous glucocorticoids and increased the expression of osteogenic-related genes[5].
In vivo, BVT 2733 treatment via oral administration at a dose of 100mg/kg twice daily for 16 days reduced food intake and body weight gain in diet-induced obese mice[6]. Oral administration of BVT 2733 (100mg/kg) twice daily for 2 weeks alleviated collagen-induced arthritis in mice and reduced the levels of TNF-α, IL-1β, IL-6, and IL-17 in serum[7]. Subcutaneous injection of BVT 2733 (167mg/kg/day) for 7 days reduced the mRNA levels of hepatic glucose-6-phosphatase, as well as the blood glucose and serum insulin concentrations of spontaneously hyperglycemic KKAy mice[8].
References:
[1] Barf T, Williams M. Recent progress in 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) inhibitor development[J]. Drugs Future, 2006, 31(3).
[2] Wu D, Zhu D, Qin H, et al. 11β-HSD1 may Aggravate Sepsis-associated Endothelial Dysfunction by Activating the NF-κB/MAPK Pathway and NLRP3 Inflammasome[J]. Current Medicinal Chemistry, 2026.
[3] Qi W, Liu Y, Liu P, et al. 11β-hydroxysteroid dehydrogenase type 1 selective inhibitor alleviates insulin resistance and non-alcoholic fatty liver disease in db/db mice[J]. ScienceAsia, 2024, 50(1): 10.2306.
[4] Luo L, Zhu D, Zhang Z, et al. 11β-Hydroxysteroid dehydrogenase type 1 amplifies inflammation in LPS-induced THP-1 cells[J]. Iranian Journal of Basic Medical Sciences, 2023, 26(3): 374.
[5] Wu L, Qi H, Zhong Y, et al. 11β-Hydroxysteroid dehydrogenase type 1 selective inhibitor BVT. 2733 protects osteoblasts against endogenous glucocorticoid induced dysfunction[J]. Endocrine Journal, 2013, 60(9): 1047-1058.
[6] Wang S J Y, Birtles S, De Schoolmeester J, et al. Inhibition of 11β-hydroxysteroid dehydrogenase type 1 reduces food intake and weight gain but maintains energy expenditure in diet-induced obese mice[J]. Diabetologia, 2006, 49(6): 1333-1337.
[7] Zhang L, Dong Y, Zou F, et al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis[J]. International immunopharmacology, 2013, 17(3): 489-494.
[8] Alberts P, Engblom L, Edling N, et al. Selective inhibition of 11β-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice: P. Alberts et al.: 11β-HSD1 inhibition lowers blood glucose[J]. Diabetologia, 2002, 45(11): 1528-1532.
| Cell experiment [1]: | |
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Cell lines |
THP-1 cells |
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Preparation Method |
THP-1 cells were cultured in RPMI-1640 medium, supplemented with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin, at 37°C in an incubator with 5% CO2. THP-1 cells were seeded into 12-well plates at a density of 5×105 cells/ml and incubated for 6h at 37°C. The cells were incubated with or without BVT 2733 one hour before LPS treatment. The cells in the LPS and LPS+BVT 2733 groups were treated with LPS for 6h at 37°C. Intracellular ROS levels were detected. |
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Reaction Conditions |
100µM; 1h |
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Applications |
BVT 2733 treatment reduced intracellular ROS levels in THP-1 cells exposed to LPS. |
| Animal experiment [2]: | |
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Animal models |
Male DBA/1 mice |
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Preparation Method |
Male DBA/1 mice (8 weeks old; 18-22g) were housed under standard conditions [temperature (22-24°C) and humidity (40-60%), a 12h light/dark cycle] with ad libitum access to food and normal drinking water. Mice were immunized intradermally at the base of the tail with 100μg of bovine type II collagen (CII) emulsified with an equal volume of complete Freund's adjuvant. DBA/1 mice were boosted 21 days after immunization by intradermal injection with 100μg of CII emulsified with incomplete Freund's adjuvant. Mice were examined for signs of joint inflammation and scored as follows: 0: no change, 1: significant swelling and redness of one digit, 2: mild swelling and erythema of the limb or swelling of more than two digits, 3: marked swelling and erythema of the limb, and 4: maximal swelling and redness of the limb and, later, ankylosis. BVT 2733 was dissolved in 12% β-hydroxypropylcyclodextrin and 0.3% sodium chloride. BVT 2733 was administered by oral gavage twice daily. Mice received BVT 2733 (100mg/kg; orally) or vehicle twice daily, starting from 24 days after the first immunization (3 days after boosted immunization) for 2 weeks. The control mice were injected with vehicle alone. Mice were sacrificed, and the hind paws were collected for analysis. |
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Dosage form |
100mg/kg; twice daily; 2 weeks; p.o. |
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Applications |
BVT 2733 treatment attenuated arthritis severity and reduced joint destruction in the hind paws of mice. |
References: [1] Luo L, Zhu D, Zhang Z, et al. 11β-Hydroxysteroid dehydrogenase type 1 amplifies inflammation in LPS-induced THP-1 cells[J]. Iranian Journal of Basic Medical Sciences, 2023, 26(3): 374. [2] Zhang L, Dong Y, Zou F, et al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis[J]. International immunopharmacology, 2013, 17(3): 489-494. | |
| Cas No. | 376640-41-4 | SDF | |
| Chemical Name | 3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide | ||
| Canonical SMILES | CC1=C(Cl)C=CC=C1S(NC2=NC(CC(N3CCN(CC3)C)=O)=CS2)(=O)=O | ||
| Formula | C17H21ClN4O3S2 | M.Wt | 428.96 |
| Solubility | ≥ 42.9mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3312 mL | 11.6561 mL | 23.3122 mL |
| 5 mM | 466.2 μL | 2.3312 mL | 4.6624 mL |
| 10 mM | 233.1 μL | 1.1656 mL | 2.3312 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)