1. MAPK/ERK Pathway
  2. MEK
  3. PD 198306

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。

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PD 198306 Chemical Structure

PD 198306 Chemical Structure

CAS No. : 212631-61-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.

纯度 & 产品资料
参考文献

PD 198306 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PD 198306
目录号:
HY-107620
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