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CAS No.: 449811-01-2

Pamapimod Catalog No. CSN19013

Synonyms: Ro4402257;R1503

Pamapimod is a selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 mM, respectively with no activity against p38delta or p38gamma isoforms.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The family members of the mitogen-activated protein kinase (MAPK) mediate a wide variety of cellular behaviors in response to extracellular stimuli. One of the four main sub-groups, the p38 group of MAP kinases, serve as a nexus for signal transduction and play a vital role in numerous biological processes^[3]. Pamapimod inhibited p38α and p38β enzymatic activity, with IC₅₀ values of 0.014 ± 0.002 and 0.48 ± 0.04 μM, respectively^[4]. Pamapimod inhibited p38 (IC₅₀, 0.06 μM), but inhibition of c-Jun NH(2)-terminal kinase (JNK) was not detected. Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF)-α production by monocytes, interleukin (IL)-1β production in human whole blood, and spontaneous TNFα production by synovial explants from rheumatoid arthritis (RA) patients^[4]. Intravenous systemic clearance of pamapimod was low to moderate across species pamapimod was well absorbed and had high oral bioavailability in the rat, monkey, and dog (62%-80%)^[5]. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod. In murine collagen-induced arthritis, pamapimod reduced clinical signs of inflammation and bone loss at 50 mg/kg or greater. In a rat model of hyperalgesia, pamapimod increased tolerance to pressure in a dose-dependent manner, suggesting an important role of p38 in pain associated with inflammation^[4]. we treated ovariectomized (OVX) mice with pamapimod and revealed a protective effect of pamapimod on osteoporosis in vivo^[6].
动物研究
剂量
Rat: 10 mg/kg - 100 mg/kg^[3] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Rat: 10 mg/kg - 100 mg/kg^[3] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4607 mL
- 12.3037 mL
- 24.6073 mL
- 5 mM
- 0.4921 mL
- 2.4607 mL
- 4.9215 mL
- 10 mM
- 0.2461 mL
- 1.2304 mL
- 2.4607 mL

技术信息

CAS号

449811-01-2

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H20F2N4O4

运输

蓝冰

分子量

406.38

别名

Ro4402257;R1503

溶解度

DMSO	79.0 mg/mL (194.4 mM)
Water	Insoluble
Ethanol	28.0 mg/mL (68.9 mM)

动物实验配方

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