• 产品描述： BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency

• 靶点： HDAC3:54 nM (IC50);HDAC3:29 nM (Ki);HDAC1:1260 nM (IC50);HDAC1:5100 nM (Ki);HDAC2:1340 nM (IC50);HDAC2:6300 nM (Ki);HIV-1;Apoptosis; HIVProtease; HDAC

• 体外研究：
  BRD3308 (5-30 μM；6-24 小时) 处理增加 2D10 细胞系中的 HIV-1 表达。 BRD3308 (15 μM；过夜) 能够诱导生长静息 CD4+ T 细胞中来自体外潜伏感染细胞的 HIV-1。BRD3308 抑制 HDAC1、HDAC2 和 HDAC3，Ki 值分别为 5.1 μM、6.3 μM 和 29 nM RT-PCR Cell Line: 2D10 cells Concentration: 5 µM, 10 µM, 15 µM, or 30 µM Incubation Time: 6 hours, 12 hours, 18 hours, or 24 hours Result: An increase in HIV-1 expression was observed.

• 体内研究：
  BRD3308 (5 mg/kg；腹膜内注射；每隔一天；雄性 Zucker 糖尿病肥胖大鼠) 处理可降低 2 型糖尿病大鼠模型中的高血糖并增加胰岛素分泌。在高血糖钳夹结束时，BRD3308 处理大鼠的循环胰岛素水平显著升高。胰腺胰岛素染色和含量也显著升高。BRD3308 在体内保持功能性 β 细胞团抵抗糖脂毒性。 Animal Model: Male Zucker Diabetic Fatty (Obese) rats (6-week-old) Dosage: 5 mg/kg Administration: Intraperitoneal injection; every second day Result: Reduced hyperglycaemia and increased insulin secretion in a rat model of type 2 diabetes.

• 参考文献：
  1. Barton KM, et al. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014 Aug 19;9(8):e102684. 2. Lundh M, et al. Histone deacetylase 3 inhibition improves glycaemia and insulin secretion in obese diabetic rats. Diabetes Obes Metab. 2015 Jul;17(7):703-7. 3. Wagner FF, et al. An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. ACS Chem Biol. 2016 Feb 19;11(2):363-74.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.481 ml	17.404 ml	34.808 ml
  5 mM	0.696 ml	3.481 ml	6.962 ml
  10 mM	0.348 ml	1.74 ml	3.481 ml
  50 mM	0.07 ml	0.348 ml	0.696 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *