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Pamapimod (R-1503, Ro4402257)
目录号: PC11802 纯度: ≥98%
CAS No. :449811-01-2
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PC11802-10mM (in 1mL DMSO) 10mM(in1mLDMSO) ¥5192.00 请登录
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中文名称
Pamapimod (R-1503, Ro4402257)
中文别名
6-(2,4-二氟苯氧基)-2-[(1,5-二羟基-3-戊烷基)氨基]-8-甲基吡啶并[2,3-d]嘧啶-7(8H)-酮;N-(8-苄基-8-氮杂双环[3.2.1]辛-3-基-外向)-2-甲基丙酰胺;帕吡莫德
英文名称
Pamapimod (R-1503, Ro4402257)
英文别名
Pyrido[2,3-d]pyrimidin-7(8H)-one,6-(2,4-difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methyl-;Pamapimod;6-(2,4-difluorophenoxy)-2-(1,5-dihydroxypentan-3-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-one;R1503;Ro4402257;RO 4402257;8S2C9V11K4;R 1503;6-(2,4-Difluorophenoxy)-2-{[3-Hydroxy-1-(2-Hydroxyethyl)propyl]amino}-8-Methylpyrido[2,3-D]pyrimidin-7(8h)-One;Pamapimod [USAN:INN];6-(2,4-Difluorophenoxy)-2-((3-hydroxy-1-(2-hydroxyethyl)propyl)amino)-8-methylpyrido(2,3-d)pyrimidin-7(8H)-one;6-(2,4-Difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methylpyrido[2,3-d]pyrimidin
Cas No.
449811-01-2
分子式
C19H20F2N4O4
分子量
406.38
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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.

性状

Solid

IC50 & Target[1][2]

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.
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.

Medlife 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.

Medlife 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.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 34 mg/mL (83.67 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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