Foliglurax-PXT002331-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFoligluraxCat. No.: HY-108703CAS No.: 1883329-51-8Synonyms: PXT002331分式: CHNOS分量: 421.51作靶點(diǎn): mGluR作通路: GPCR/G Protein; Neuronal Signaling儲存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)體外實驗 DMSO : 5

2、.2 mg/mL (12.34 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3724 mL 11.8621 mL 23.7242 mL5 mM 0.4745 mL 2.3724 mL 4.7448 mL10 mM 0.2372 mL 1.1862 mL 2.3724 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果

3、的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.52 mg/mL (1.23 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.52 mg/mL (1.23 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Maste

4、r of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Foliglurax (PXT002331)種可滲透腦的，有效的選擇性代謝型氨酸受體 4 正變構(gòu)調(diào)節(jié)劑 (mGluR4PAM)，EC50 為 79 nM 1?？古辽?1。IC50 & Target mGlu479 nM (EC50)體外研究 Foliglurax, a highly selective and potent mGlu4 receptor PAM with a marked brain-penetrance feature, mightrevolutionize the field of m

5、Glu4 receptor drug targeting in CNS disorders 2.REFERENCES1. Charvin D, et al. Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Seriesof Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4. J Med Chem. 2017 Oct 26;60(20):8515-8537.2. Volpi C, et al. Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4. Expert Opin Drug Discov.2018 May;13(5):411-423.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-