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(1R,2S)-VU0155041

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Chemical Structure| 1263273-14-8 同义名 : -
CAS号 : 1263273-14-8
货号 : A1177247
分子式 : C14H15Cl2NO3
纯度 : 95%
分子量 : 316.18
MDL号 : MFCD26142602
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(158.14 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 The Cis regioisomer of VU0155041 demonstrates similar potency, with 798±58 nM at human mGluR4 and 693±140 nM at rat mGluR4. In contrast, the concentration-response curve for the Trans regioisomer (VU0155040) does not plateau at the maximum concentration tested. At 30 μM, the Cis regioisomer of VU0155041 is more effective in inducing shifts in baseline in fold-shift experiments using the thallium flux assay, reaching about 45% of the maximal response seen with glutamate. VU0155041 acts as a partial agonist of mGluR4 by interacting with a site distinct from the glutamate binding site and shows selectivity for mGluR4 over 67 different targets, without affecting striatal NMDA receptor function[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.81mL

3.16mL

1.58mL

31.63mL

6.33mL

3.16mL

参考文献

[1]Niswender CM, et al. Discovery, characterization, and antiparkinsonian effect of novel positiveallosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58.