BVT-2733

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

小鼠 11β-HSD1 的非甾体异构体选择性抑制剂，Ki 为 1 uM。

A non-steroidal, isoform-selective inhibitor of mouse 11β-HSD1 with Ki of 1 uM; displays >20-fold selectivity over 11β-HSD2; lowers hepatic PEPCK and glucose-6-phosphatase mRNA, blood glucose and serum insulin concentrations in a hyperglycaemic and hyperinsulinaemic mouse model.Diabetes Preclinical(In Vitro):BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 μM) reduces MCP-1 expression in fully differentiation adipocytes.BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium in J774.1 macrophages by Elisa.(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.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.

BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 μM) reduces MCP-1 expression in fully differentiation adipocytes.BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium?in J774.1 macrophages by Elisa. RT-PCRCell Line:Differentiation adipocytes Concentration:100 μM Incubation Time:24 hours Result:Down-regulated MCP-1 mRNA level.

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.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. Animal Model:Collagen-induced arthritis (CIA)?miceDosage:100 mg/kg Administration:Oral administration; twice daily; 2 weeks Result:Reduced synovial inflammation and joint destruction.Animal Model:C57BL/6J miceDosage:100 mg/kg Administration:Oral administration; dosed (09.00 and 17.00 h); last 4 weeks Result:Improved metabolic homeostasis and suppressed the inflammation of adipose tissue in diet-induced obese mice.?

BVT2733 | BVT 2733

Metabolic Enzyme/Protease

11β-HSD

11β-HSD1

Metabolic Disease

Diabetes

376640-41-4

428.9566

C17H21ClN4O3S2

>98% (HPLC)

10 mM in DMSO

CN1CCN(C(CC2=CSC(NS(=O)(C3=CC=CC(Cl)=C3C)=O)=N2)=O)CC1

Benzenesulfonamide, 3-chloro-2-methyl-N-[4-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]-2-thiazolyl]-

(-20℃)

With Ice Pack

≥ 2 years