BRD6688
目录号 : GC13088
A kinetically selective HDAC2 inhibitor
Cas No.:1404562-17-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 21 nM, 100 nM, and 11.48 μM for HDAC1, 2, and 3, respectively
BRD6688 is an HDAC inhibitor.
A few chromatin modifying enzymes have been implicated in the neurobiology of learning and memory, especially, histone deacetylases (HDACs). HDACs are responsible for catalyzing the posttranslational hydrolysis of acetyl groups from the 3-nitrogen of lysine residues of histone and non-histone proteins.
In vitro: BRD6688 was found to demonstrate kinetic selectivity for HDAC2 against HDAC1, an isoform with 95% similarity within the catalytic binding domain. Moreover, BRD6688 could increase histone acetylation (H4K12 and H3K9) in primary mouse neuronal cultures [1].
In vivo: Mouse in-vivo study showed that BRD6688 was able to increase the histone acetylation (H4K12 and H3K9) in hippocampal CA1 neurons of CK-p25 mice. Moreove, the increased histone acetylation in brain served as a surrogate pharmacodynamic marker of HDAC engagement and was consistent with previously observed brain pharmacokinetic properties. In addition, BRD6688 rescued the cognitive deficits in CK-p25 mice, a model of neurodegeneration, in a Pavlovian fear conditioning behavioral assay [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Wagner, F. F.,Zhang, Y.-L.,Fass, D.M., et al. Kinetically selective inhibitors of histone deacetylase 2 (HDAC2) as cognition enhancers. Chem.Sci. 6(1), 804-815 (2015).
| Cas No. | 1404562-17-9 | SDF | |
| 化学名 | N-[2-amino-5-(4-pyridinyl)phenyl]-1-pyrrolidinecarboxamide | ||
| Canonical SMILES | O=C(N1CCCC1)NC2=CC(C3=CC=NC=C3)=CC=C2N | ||
| 分子式 | C16H18N4O | 分子量 | 282.3 |
| 溶解度 | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5423 mL | 17.7117 mL | 35.4233 mL |
| 5 mM | 0.7085 mL | 3.5423 mL | 7.0847 mL |
| 10 mM | 0.3542 mL | 1.7712 mL | 3.5423 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。