中文名称: | ADX71743 | ||||
---|---|---|---|---|---|
英文名称: | ADX71743 | ||||
别名: | 6-(2,4-Dimethylphenyl)-2-ethyl-4,5,6,7-tetrahydro-1,3-benzoxazol-4-one | ||||
CAS No: | 1431641-29-0 | 分子式: | C17H19NO2 | 分子量: | 269.34 |
CAS No: | 1431641-29-0 | ||||
分子式: | C17H19NO2 | ||||
分子量: | 269.34 |
包装规格:
5mg in glass bottle
产品简介:
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。
溶解性:
溶于DMSO(5mg/mL 加热)
靶点:
mGlu7
体外研究:
ADX71743 has an IC50 of 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.
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.
ADX71743 can against an EC80 of glutamate (IC50 of 22 nM) as well as against an EC80 of L-AP4 (IC50 of 125 nM).
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.
ADX71743 can against an EC80 of glutamate (IC50 of 22 nM) as well as against an EC80 of L-AP4 (IC50 of 125 nM).
体内研究:
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).
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
保存条件:
-20℃
注意事项:
1、为了您的安全和健康,请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码:
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危害声明:
安全说明:
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