产品
编 号:F271923
分子式:C18H16F3IN2O2
分子量:476.23
产品类型
结构图
CAS No: 212631-61-3
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产品详情
生物活性:
PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects.
体内研究:
Intrathecal administration of PD 198306 (1-30 μg per 10 μL) dose-dependently (1-30 μg) blocks static allodynia in both the streptozocin and the chronic constriction injury (CCI) models of neuropathic pain.Animal Model:Male Sprague Dawley rats (250-300 g) bearing neuropathic pain
Dosage:1-30 μg per 10 μL and 3 mg per 100 μL (PD 198306 is suspended in cremophor:ethanol:water, 1 : 1 : 8.)
Administration:Single doses of intrathecal (i.t.) or intraplantar (ipl) of PD 198306 (1-30 μg per 10 μL and 3 mg per 100 μL respectively
Result:Intrathecal administration dose-dependently (1-30 μg) blocked static allodynia the streptozocin model of neuropathic pain. The minimum effective doses (MED) of 3 μg significantly blocked static allodynia 30 min after treatment. Both 10 μg and the highest dose used (30 μg) totally blocked the maintenance of static allodynia, for up to 1 h.
体外研究:
PD198306 significantly inhibits Tha-GFP replication by 25% at 10?μM, after 36?h.PD198306 (5?μM) reduces Tha-Crimson replication significantly by 20% at 18?h but such a result could not be confirmed at 36?h.