BMT-145027 - CAS:2018282-44-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	BMT-145027
英文名称:	BMT-145027
别名:	BMT-145027 3-[4-Chloro-3-(trifluoromethyl)phenyl]-4-cyclopropyl-6-phenyl-2H-pyrazolo[3,4-b]pyridine-5-carbonitrile
CAS No:	2018282-44-3	分子式:	C₂₃H₁₄ClF₃N₄	分子量:	438.83
CAS No:	2018282-44-3
分子式:	C₂₃H₁₄ClF₃N₄
分子量:	438.83

点击下载产品说明书(PDF)

B11687 BMT-145027 ≥98% (psaitong)

相关产品

包装规格：

5mg 10mg 50mg in glass bottle

溶解性：

溶于DMSO(2mg/mL超声加热）

产品描述：

基本信息

产品编号：	B11687
产品名称：	BMT-145027
CAS:	2018282-44-3	储存条件	粉末	-20℃	四年

分子式：	C23H14ClF3N4		溶于液体	-80℃	6个月
分子量：	438.83			-20℃	1个月
化学名：	3-[4-Chloro-3-(trifluoromethyl)phenyl]-4-cyclopropyl-6-phenyl-2H-pyrazolo[3,4-b]pyridine-5-carbonitrile
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜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。

制备储备液

浓度

溶液体积

质量

1mg

5mg

10mg

1mM

2.2788mL

11.3939mL

22.7879mL

5mM

0.4558mL

2.2788mL

4.5576mL

生物活性

产品描述	一种mGluR5 的正变构调节物且没有固有的激动剂活性，EC50值为47nM。
靶点	mGluR5 47nM (EC50)
体外研究	BMT-145027 is a compound with high MsLM stability (85% remaining),acceptable potency (EC50=47nM),and a modest decrease in planarity (Fsp3=0.17).Importantly,BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16μM.
体内研究	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 30mg/kg,with an apparent trend in novel object preference at 10mg/kg.Satellite animals indicates a total plasma concentration of 2800nM at 30mg/kg.

推荐实验方法(仅供参考)

激酶实验：

Competition binding experiments are performed using a single concentration ( 5nM) of [3H]-MethoxyPyEP in the presence of increasing concentrations of BMT-145027.The reaction is terminated by the addition of 5mL 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 8h and then read on the micro-beta counter.IC50 values are determined using non-linear regression four-parameter logistic equation.

动物实验:
Mice:Mice are dosed i.p.with either vehicle or BMT-145027 at 10 and 30mg/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.