1R-2S-VU0155041-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE(1R,2S)-VU0155041Cat. No.: HY-14417ACAS No.: 1263273-14-8分式: CHClNO分量: 316.18作靶点: mGluR作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 59 mg/mL (186.6

2、0 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1628 mL 15.8138 mL 31.6276 mL5 mM 0.6326 mL 3.1628 mL 6.3255 mL10 mM 0.3163 mL 1.5814 mL 3.1628 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 (1R,2S)-VU0155041是VU0155041的顺式异构体。(1R

3、,2S)-VU0155041是mGluR4的部分激动剂，EC50值为2.35 M。IC50 & Target EC50: 2.35 M (rat mGluR4) 1体外研究At both human and rat receptors, the Cis regioisomer of VU0155041 is similar in potency (79858 nM at1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEhuman mGluR4 and 693140 nM at rat mGluR4). Conversely, the concen

4、tration-response curve for theTrans regioisomer (VU0155040) does not plateau at the maximum concentration tested. Fold-shiftexperiments at 30 M of VU0155041 also shows that the Cis regioisomer is more effective at thisconcentration on both human and rat mGluR4. VU0155041, induces concentration-depen

5、dent shifts in thebaseline when examined in fold shift experiments using the thallium flux assay. VU0155041 induces aresponse that reaches approximately 45% of the maximal glutamate response. VU0155041is a partialagonist of mGluR4 that activates the receptor by interacting with a site that is distin

6、ct from the glutamatebinding site. VU0155041 exhibitsselectivity for mGluR4 relative to 67 different targets and does not affect thefunction of striatal NMDA receptors 1.体内研究 VU0155041 is soluble in an aqueous vehicle and intracerebroventricular administration of 31 to 316 nM ofVU0155041 dose-depend

7、ently decreases haloperidol-induced catalepsy and reserpine-induced akinesia inrats. VU0155041, at doses of 31 and 92 nmol, is also able to significantly decrease the cataleptic effects ofhaloperidol, and the effects of the compound are still present 30 min after infusion. Icv infusion of a 316 nmol

8、dose of VU0155041 also results in a significant reversal of akinesia 1.PROTOCOLAnimal Rats: TVC rats are injected with reserpine and kept in their home cages for 2 hr after injection. Activity isAdministration 1 measured by placing rats in photocell activity cages equipped with 1616 infrared beams.

9、After a 30 minbaseline period, rats are given a single intracerebroventricular injection of either L-AP4 (100, 300 or 1000nM), VU0155041 (93 or 316 nM), or corresponding vehicles, and motor activity is recorded for an additional30 min 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Niswender CM, et al. Discovery, characterization, and antiparkinsonian effect of novel positiveallosteric modulators of metabotropicglutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58.McePdfHeightCaution: Product has not been fully validat