Pamapimod

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Pamapimod

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。

CAS NO:

449811-01-2

Ro4402257
R1503

Pamapimod (Ro4402257) 是一种有效的，选择性和口服活性的p38 MAPK抑制剂，对于p38α和p38β的IC₅₀分别为 14 nM 和 480 nM，K_i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。

生物活性

Pamapimod (Ro4402257) is a potent, selective and orally activep38 MAPKinhibitor withIC₅₀s of 14 nM and 480 nM andK_is of 1.3 nM and 120 nM forp38αandp38β, respectively. Pamapimod has no activity againstp38δorp38γisoforms. 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 K_ivalues 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 EC₅₀of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC₅₀values of 0.40 and 0.10 μM, respectively^[1].

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].

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

性状

Solid

Formula

C₁₉H₂₀F₂N₄O₄

CAS 号

449811-01-2

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。