BVT 2733 |
| رقم الكتالوجGC15738 |
يعتبر BVT 2733 مثبطًا قويًا وانتقائيًا ونشطًا عن طريق الفم غير ستيرويدي 11β-hydroxydehydrogenase 1 (11β-HSD1)
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 novel, small-molecule, nonsteroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with IC50 of 96 nM (mice)[1].
BVT 2733 attenuated the mRNA levels of MCP-1 and IL-6 in PA or LPS treated J774A.1 macrophages. The protein levels of MCP-1 and IL-6 in the medium were also attenuated[2]. After constructing the mouse 11β-HSD1 overexpression lentiviral vector, MC3T3-E1 preosteoblasts were infected with negative control lentivirus and overexpressing 11β-HSD1 lentivirus, respectively, and then added with the selective inhibitor of 11β-HSD1 BVT 2733 to reverse the inhibitory effect of 11β-HSD1 expression on osteogenesis[6]. A significant increase in the expression of BAT-specific genes, including UCP1, Cidea, Cox7a1 and Cox8b, was observed in BVT 2733 treated and 11β-HSD1-deficient mouse native brown adipocytes[7].
BVT 2733 administration normalized the expression profile of adiponkines by up-regulating the mRNA levels of adiponectin and vaspin and down-regulating the expression of resistin in adipose tissue. In line with these changes in adipose tissue serum levels of adiponectin and leptin were also improved by BVT 2733 treatment[2]. BVT 2733 treatment attenuated the arthritis severity and anti-CII level in CIA mice. BVT-2733 also decreased the levels of serum TNF-α, IL-1β, IL-6 and IL-17. BVT 2733 treatment also significantly reduced synovial inflammation and joint destruction[3]. In hyperglycemic, but not in normal mice, BVT 2733 lowered circulating glucose and insulin levels. In oral glucose tolerance tests in ob/ob and KKAy mice, glucose concentrations were 65-75% of vehicle values after BVT 2733 treatment, and in KKAy mice insulin concentrations were decreased[4]. BVT 2733 reduced food intake but prevented a concomitant reduction in lean body mass and energy expenditure. The latter effects may have contributed to improved glucose tolerance[5].
References:
[1]: Alberts P, Engblom L, et,al. Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice. Diabetologia. 2002 Nov;45(11):1528-32. doi: 10.1007/s00125-002-0959-6. Epub 2002 Sep 18. PMID: 12436336.
[2]: Wang L, Liu J, 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. doi: 10.1371/journal.pone.0040056. Epub 2012 Jul 2. PMID: 22768329; PMCID: PMC3388048.
[3]: Zhang L, Dong Y, et,al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis. Int Immunopharmacol. 2013 Nov;17(3):489-94. doi: 10.1016/j.intimp.2013.07.015. Epub 2013 Aug 11. PMID: 23938253.
[4]: Alberts P, Nilsson C, et,al. Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains. Endocrinology. 2003 Nov;144(11):4755-62. doi: 10.1210/en.2003-0344. Epub 2003 Jul 31. PMID: 12960099.
[5]: Wang SJ, Birtles S, et,al. Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 reduces food intake and weight gain but maintains energy expenditure in diet-induced obese mice. Diabetologia. 2006 Jun;49(6):1333-7. doi: 10.1007/s00125-006-0239-y. Epub 2006 Apr 13. PMID: 16612591.
[6]: Wu L, Qi H, et,al. 11β-Hydroxysteroid dehydrogenase type 1 selective inhibitor BVT.2733 protects osteoblasts against endogenous glucocorticoid induced dysfunction. Endocr J. 2013;60(9):1047-58. doi: 10.1507/endocrj.ej12-0376. Epub 2013 Jun 12. PMID: 23759754.
[7]: Liu J, Kong X, et,al. Essential roles of 11β-HSD1 in regulating brown adipocyte function. J Mol Endocrinol. 2013 Jan 11;50(1):103-13. doi: 10.1530/JME-12-0099. PMID: 23197361.
| Cell experiment [1]: | |
Cell lines | Mouse reticulum cell sarcoma-derived cell, J774.1 |
Preparation Method | J774.1 macrophages were activated by PA or LPS and co-treated with 11β-HSD1 inhibitor BVT 2733 (25-100 µmol/L) for 24 h. |
Reaction Conditions | 25-100 µM BVT 2733 for 24h |
Applications | BVT 2733 attenuated the mRNA levels of MCP-1 and IL-6 in PA or LPS treated J774A.1 macrophages. The protein levels of MCP-1 and IL-6 in the medium were also attenuated. |
| Animal experiment [1]: | |
Animal models | Male C57BL/6J mice at age of 18 days |
Preparation Method | From 3 weeks of age, all mice were fed with a normal chow diet containing 10% calory from fat (NC mice), or a high fat diet (HFD) containing 50% calorie from fat for 24 weeks. During the last four weeks the HFD-fed mice were dosed with BVT 2733 (100 mg/kg, orally) (HFD+BVT mice) or vehicle (HFD mice). |
Dosage form | BVT 2733 (100 mg/kg, orally) for 4 weeks |
Applications | BVT 2733 administration normalized the expression profile of adiponkines by up-regulating the mRNA levels of adiponectin and vaspin and down-regulating the expression of resistin in adipose tissue. In line with these changes in adipose tissue serum levels of adiponectin and leptin were also improved by BVT 2733 treatment. |
References: | |
| 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 |
| الذوبان | ≥ 42.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3312 mL | 11.6561 mL | 23.3122 mL |
| 5 mM | 0.4662 mL | 2.3312 mL | 4.6624 mL |
| 10 mM | 0.2331 mL | 1.1656 mL | 2.3312 mL |
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