Mardepodect

A potent inhibitor of PDE10A

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2mg

￥1212.00

970.00

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5mg

￥1525.00

1220.00

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10mg

￥2875.00

2300.00

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50mg

￥7537.00

6030.00

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100mg

￥11875.00

9500.00

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200mg

￥0.00

0.00

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500mg

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0.00

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货号: ajce57322
CAS: 898562-94-2
别名: 2-[[4-[1-甲基-4-(4-吡啶基)-1H-吡唑-3-基]苯氧基]甲基]-喹啉,PF-2545920
分子式: C25H20N4O
分子量: 392.45
纯度: >98%
溶解度: DMSO: ≥ 45 mg/mL (114.66 mM)
储存: Store at -20°C
库存: 现货

Background

PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC₅₀ = 1.26 nM for the human recombinant enzyme).¹ It is selective for PDE10A over other PDEs with IC₅₀ values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine in mice (ID₅₀ = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID₅₀s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington's disease.

1.Grauer, S.M., Pulito, V.L., Navarra, R.L., et al.Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophreniaJ. Pharmacol. Exp. Ther.331(2)574-590(2009)