BRD-6929|cas:849234-64-6|西域试剂

BRD-6929,99.04%

产品编号：Bellancom-100719| CAS NO：849234-64-6| 分子式：C₁₉H₁₇N₃O₂S| 分子量：351.42

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100719	￥900.00	杭州北京（现货）
Bellancom-100719	￥1700.00	杭州北京（现货）
Bellancom-100719	￥3700.00	杭州北京（现货）
Bellancom-100719	￥6500.00	杭州北京（现货）
Bellancom-100719	￥11500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

BRD-6929

产品介绍

BRD-6929 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 (K_i = 0.2 和 1.5 nM)。BRD-6929 可用于情绪相关行为的研究。

生物活性

BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC₅₀ of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with K_i of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research.

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 (K_i) and kinetics (half-life ‘T_1/2′ in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 µM), the K_i values are <0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T_1/2 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

BRD-6929 (intraperitoneal injection; 45 mg/kg; single dose) exhibits a C_max, T_1/2 and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a C_max, T_1/2 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (14.23 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8456 mL	14.2280 mL	28.4560 mL
5 mM	0.5691 mL	2.8456 mL	5.6912 mL
10 mM	0.2846 mL	1.4228 mL	2.8456 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

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); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.92 mM，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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明