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BRD-6929  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：是 I 类组蛋白去乙酰化酶 HDAC1 和 HDAC2 的脑渗透性选择性抑制剂 (IC50= 1 和 8 nM)。BRD-6929 对 HDAC1 和 HDAC2 有高亲和力 (Ki = 0.2 和 1.5 nM)。BRD-6929 可用于情绪相关行为的研究。
溶解性：溶于DMSO（5 mg/mL 超声)
储备液保存：-80°C, 6 months -20°C, 1 month
体内实验：1、请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in Saline) Solubility: ≥ 2.08 mg/mL (5.92 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
靶点：HDAC1：1 nM (IC50) HDAC2：8 nM (IC50) HDAC3：458 nM (IC50) HIV-1
体外研究：In vitro IC50 for HDAC1-9 by BRD-6929 using recombinant human HDAC enzymes and HDAC class-specific substrates. BRD-6929 and substrate are incubated for 180 min (HDAC1-3) to control for HDAC1-3 inhibition, BRD-6929 is against HDAC1, HDAC2, HDAC3 and HDAC4-9 with IC50s of 0.001 µM, 0.008 µM, 0.458 µM and >30 µM, respectively. In vitro binding affinity (Ki) and kinetics (half-life ‘T1/2′ in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 µM), the Ki values are <0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T1/2 values are >2400 mins, >4800 mins, and 1200 mins for HDAC 1, 2 and 3, respectively. BRD-6929 (1 and 10 uM) does not cause an increase or decrease in overall cell number in brain region specific primary cultures. Additionally, BRD-6929 (10 uM) causes an increase in H4K12 acetylation in brain region specific primary cultures (striatum). BRD-6929 (1-10 uM; 6 hours) causes a significant increase in H2B acetylation in primary neuronal cell cultures. BRD-6929 (1-20 uM; 24 hours) induces a dose-dependent acetylation of H4K12ac with an EC50 of 7.2 µM in cultured neurons. BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1.
体内研究：BRD-6929 (intraperitoneal injection; 45 mg/kg; single dose) exhibits a Cmax, T1/2 and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a Cmax, T1/2 and AUC values of 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively in brain. BRD-6929 (intraperitoneal injection; 45 mg/kg; 10 days) acts as a deacetylase inhibitor in mouse brain. It significantly increases acetylation in each brain region by 1.5- to 2.0-fold compared to vehicle. The western blotting reveals that BRD-6929 significantly increases acetylation of histone H2B (tetra-acetylated), H3K9 and H4K12 in cortex, ventral striatum and hippocampus after the 10th daily treatment in adult male C57BL/6J mice.
保存条件：-20℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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