| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
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).
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 ?mol/L) for 24 h. |
Reaction Conditions |
25-100 ?M 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 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. |
| 半岛bd体育手机客户端 描述 | 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: |
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