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PD 198306
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD 198306图片
CAS NO:212631-61-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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].

IC50& Target[1]

MEK

 

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.
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.
分子量

476.23

Formula

C18H16F3IN2O2

CAS 号

212631-61-3

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.