Pamapimod Ro4402257; R1503|cas:449811-01-2|西域试剂

Pamapimod Ro4402257; R1503,99.92%

产品编号：Bellancom-10405| CAS NO：449811-01-2| 分子式：C₁₉H₂₀F₂N₄O₄| 分子量：406.38

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货号	价格	库存与货期
Bellancom-10405	￥3200.00	杭州北京（现货）
Bellancom-10405	￥5800.00	杭州北京（现货）
Bellancom-10405	￥10000.00	杭州北京（现货）
Bellancom-10405	￥0.00	杭州北京（现货）

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Pamapimod Ro4402257; R1503

产品介绍

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 active p38 MAPK inhibitor with IC₅₀s of 14 nM and 480 nM and K_is 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.

体外研究

Pamapimod binds to JNK kinases with K_i values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively.
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.

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

体内研究

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

西域 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
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.

体内研究

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

西域 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
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.

性状

Solid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式