| Bioactivity | 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[1]. | ||||||||||||
| Target | IC50: 96 nM (mouse 11β-HSD1)IC50: 3341 nM (human 11β-HSD1) | ||||||||||||
| Invitro | 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]. RT-PCR[3] Cell Line: | ||||||||||||
| In Vivo | BVT-2733 (oral administration; 100 mg/kg; twice daily; 2 weeks) attenuates the arthritis severity and anti-CII level and decreases the levels of serum TNF-α, IL-1β, IL-6 and IL-17 in CIA mice[2].BVT 2733 (oral administration; 100 mg/kg; dosed (09.00 and 17.00 h); last 4 weeks) exhibits decreased body weight and enhanced glucose tolerance and insulin sensitivity when it compares to control mice. It also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha (TNF-α) and the number of infiltrated macrophages within the adipose tissue in vivo[3]. Animal Model: | ||||||||||||
| Name | BVT 2733 | ||||||||||||
| CAS | 376640-41-4 | ||||||||||||
| Formula | C17H21ClN4O3S2 | ||||||||||||
| Molar Mass | 428.96 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
BVT 2733
CAS: 376640-41-4 F: C17H21ClN4O3S2 W: 428.96
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT
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