PD 198306 是一种选择性 MAPK/ERK 激酶 (MEK) 抑制剂。PD 198306 显著降低 Streptozocin 诱导的 ERK1/2 水平升高。具有抗痛觉过敏作用。
| 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 activeERK1and 2. Antihyperalgesic effects[1]. |
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体外研究
(In Vitro) | PD198306 significantly inhibits Tha-GFP replication by 25% at 10 μM, after 36 h[2].
PD198306 (5 μM) reduces Tha-Crimson replication significantly by 20% at 18 h but such a result could not be confirmed at 36 h[2].
Cell Cycle Analysis[2] | Cell Line: | Human induced pluripotent stem cells (iPSC) | | Concentration: | 10 μM | | Incubation Time: | 6 hours | | Result: | Inhibited Tha-Crimson replication at 10 μM, reducing it by 30% at 18 h and 50% at 36 h. |
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体内研究
(In Vivo) | 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[1].
| Animal Model: | Male Sprague Dawley rats (250-300 g) bearing neuropathic pain[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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