您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > ADX71743
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
ADX71743
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ADX71743图片
CAS NO:1431641-29-0
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
ADX71743 是一种高度选择性，非竞争性且透过血脑屏障的代谢型谷氨酸受体 7 负变构调节剂 (mGlu7 NAM)。ADX71743 具有抗焦虑活性。
生物活性

ADX71743 is a highly selective, noncompetitive and brain-penetrantmetabotropic glutamate receptor 7negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity[1][2].

IC50& Target[1]

mGlu7

 

体外研究
(In Vitro)

ADX71743 has an IC50of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction[1].
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal[2].
ADX71743 can against an EC80of glutamate (IC50of 22 nM) as well as against an EC80of L-AP4 (IC50of 125 nM)[2].

体内研究
(In Vivo)

ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg)[2].
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T1/2of 0.68, 0.40 hours, a Cmaxof 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice[2].

Animal Model:Adult male C57Bl6/J mice (24-30 g)[2]
Dosage:50, 100, 150 mg/kg
Administration:SC
Result:Resulted in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
Animal Model:Adult male C57Bl6/J mice (24-30 g) and Sprague-Dawley rats (250-350 g)[2]
Dosage:12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis)
Administration:SC
Result:Had a T1/2of 0.68, 0.40 hours, a Cmaxof 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T1/2of 1.5 hours, a Cmaxof 16800 ng/ml of 100 mg/kg in rat.
分子量

269.34

Formula

C17H19NO2

CAS 号

1431641-29-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.