Mardepodect-hydrochloride-PF-2545920-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

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

2、性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 25 mg/mL (58.29 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)

3、驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3.25 mg/mL (7.58 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 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 您邊的抑制劑師www.MedChemE物活性 Mardepodect hydrochloride (PF-2545920 hydrochloride)種有效的選擇性 PDE10A 抑制劑，IC50 為 0.37nM，作于其他 PDE 選擇性 1000 多倍。IC50 & Target IC50: 0.37 nM (PDE10A) 1.體內(nèi)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