化合物BRD3308 T8233

Product Introduction
Bioactivity


英文名: BRD3308

描述: BRD3308 是一种高选择性的HDAC3抑制剂，IC50为 54 nM。它可激活HIV-1转录并破坏HIV-1潜伏期。它抑制由炎性细胞因子或糖脂毒性应激诱导的胰腺 β 细胞凋亡，并增加功能性胰岛素释放。

动物实验: Male Zucker Diabetic Fatty (Obese) rats (6-week-old); 5 mg/kg; Intraperitoneal injection; every second day

体内活性: BRD3308 is a selective HDAC3 inhibitor,to reduce hyperglycaemia and increase insulin secretion in a rat model of type 2 diabetes.?At diabetes onset, an ambulatory hyperglycaemic clamp was performed.?HDAC3 inhibition improved hyperglycaemia over the study period without affecting weight gain.?At the end of the hyperglycaemic clamp, circulating insulin levels were significantly higher in BRD3308-treated rats.?Pancreatic insulin staining and contents were also significantly higher.?These findings highlight HDAC3 as a key therapeutic target for β-cell protection in type 2 diabetes[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 52 mg/ml(181 mM)


关键字: β-cells | glucolipotoxicity | inflammatory | Human immunodeficiency virus | Histone deacetylases | HDAC3 | diabetes | HDAC | HIV-1 | Inhibitor | Apoptosis | latency | BRD 3308 | BRD3308 | cytokines | hyperglycaemia | HIV | inhibit | insulin | BRD-3308

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