Mardepodect-hydrochloride-PF-2545920-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMardepodect hydrochlorideCat. No.: HY-50098ASynonyms: PF-2545920 hydrochloride分式: CHClNO分量: 428.91作靶点: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解

2、性数据体外实验 DMSO : 25 mg/mL (58.29 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3315 mL 11.6575 mL 23.3149 mL5 mM 0.4663 mL 2.3315 mL 4.6630 mL10 mM 0.2331 mL 1.1657 mL 2.3315 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。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实

3、验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3.25 mg/mL (7.58 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.25 mg/mL (7.58 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Ma

4、ster of Small Molecules 您边的抑制剂师www.MedChemE物活性 Mardepodect hydrochloride (PF-2545920 hydrochloride)种有效的选择性 PDE10A 抑制剂，IC50 为 0.37nM，作于其他 PDE 选择性 1000 多倍。IC50 & Target IC50: 0.37 nM (PDE10A) 1.体内研究 The PDE10A enzyme is expressed primarily in the brain, mostly in the striatum, nucleus accumbens andolf

5、actory tubercle, and is thought to be particularly important in regulating the activity of dopamine-sensitivemedium spiny neurons in the striatum which are known to be targets of conventional antipsychotic agents. nthe conditioned avoidance response assay (CAR), Mardepodect (PF-2545920) was active w

6、ith an ED50 of 1mg/kg. Administration of Mardepodect (PF-2545920) to mice caused a dose dependent increase in striatalcGMP.REFERENCES1. Wilson JM et al. Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in dopamine D2 neuronsthan in D1 neurons in the neostriatu

7、m. Neuropharmacology. 2015 Dec;99:379-86.2. Verhoest PR et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem. 2009 Aug27;52(16):5188-96.McePdfHeightCaution: Product has not been fully validated for medical applications.For research