1. MAPK/ERK Pathway
    Autophagy
  2. p38 MAPK
    Autophagy
  3. Pamapimod

Pamapimod (Synonyms: Ro4402257; R1503)

目录号: HY-10405 纯度: 99.92%
产品使用指南

Pamapimod (Ro4402257) 是一种有效的,选择性和口服活性的 p38 MAPK 抑制剂,对于 p38αp38βIC50 分别为 14 nM 和 480 nM,Ki 分别为 1.3 nM 和 120 nM。Pamapimod 对 p38δ 或 p38γ 亚型没有活性。Pamapimod 可用于类风湿关节炎和其他自身免疫性疾病的研究。

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Pamapimod Chemical Structure

Pamapimod Chemical Structure

CAS No. : 449811-01-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3520
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5 mg ¥3200
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10 mg ¥5800
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25 mg ¥10000
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50 mg
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  • 参考文献

生物活性

Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1].

IC50 & Target[1]

p38α

14 nM (IC50)

p38α

1.3 nM (Ki)

p38β

480 (IC50)

p38β

120 nM (Ki)

体外研究
(In Vitro)

Pamapimod binds to JNK kinases with Ki values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively[1].
After lipopolysaccharide (LPS) stimulation of the human myelomonocytic cell line (THP-1), secretion of TNF-α is inhibited by Pamapimod, with an EC50 of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC50 values of 0.40 and 0.10 μM, respectively[1].

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

体内研究
(In Vivo)

Pamapimod (0-150 mg/kg; oral gavage; once daily; DBA/1J female mice) treatment reduces inflammation and bone loss in murine collagen-induced arthritis[1].

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

Animal Model: DBA/1J female mice (8-10 weeks of age) induced murine collagen[1]
Dosage: 0 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 90 mg/kg, 150 mg/kg
Administration: Oral gavage; once daily
Result: Reduced inflammation and bone loss.
分子量

406.38

Formula

C19H20F2N4O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 34 mg/mL (83.67 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4608 mL 12.3038 mL 24.6075 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 mL
10 mM 0.2461 mL 1.2304 mL 2.4608 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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目录号:
HY-10405
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