BMT-145027
目录号 : GC31081
BMT-145027是mGluR5的正变构调节物且没有固有的激动剂活性，EC50值为47nM。
Cas No.:2018282-44-3
Sample solution is provided at 25 µL, 10mM.
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BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
BMT-145027 is a compound with high MsLM stability (85% remaining), acceptable potency (EC50=47 nM), and a modest decrease in planarity (Fsp3 = 0.17). Importantly, BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16 μM[1].
Drug-treated and control mice are shown two identical objects. After a 24-h natural forgetting period, the mice are reintroduced to a familiar object while simultaneously presented with a novel object. Since mice spend more time exploring unfamiliar objects, improved memory is measured as time spent exploring the novel object. BMT-145027 leads to a significant increase in time spent with the novel object when dosed at 30 mg/kg, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals indicates a total plasma concentration of 2800 nM at 30 mg/kg[1].
[1]. Hill MD, et al. Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086.
Kinase experiment: | Competition binding experiments are performed using a single concentration ( 5 nM) of [3H]-MethoxyPyEP in the presence of increasing concentrations of BMT-145027. The reaction is terminated by the addition of 5 mL of ice-cold ish buffer and rapid filtration. The filter is punched into a 96 well flex-plate and scintillation cocktail is added to each well. The plate is allowed to soak for 8 h and then read on the micro-beta counter. IC50 values are determined using non-linear regression four-parameter logistic equation[1]. |
Animal experiment: | Mice: Mice are dosed i.p. with either vehicle or BMT-145027 at 10 and 30 mg/kg 60 min prior to the training session and tested for recognition. Animal behavior is video recorded during both training and testing and the amount of time spent exploring the objects determined using Cleversys software[1]. |
References: [1]. Hill MD, et al. Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086. | |
| Cas No. | 2018282-44-3 | SDF | |
| Canonical SMILES | ClC(C(C(F)(F)F)=C1)=CC=C1C2=NNC3=NC(C4=CC=CC=C4)=C(C#N)C(C5CC5)=C32 | ||
| 分子式 | C23H14ClF3N4 | 分子量 | 438.83 |
| 溶解度 | DMSO : 2.4 mg/mL (5.47 mM) | 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 | 2.2788 mL | 11.3939 mL | 22.7879 mL |
| 5 mM | 0.4558 mL | 2.2788 mL | 4.5576 mL |
| 10 mM | 0.2279 mL | 1.1394 mL | 2.2788 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet