Pamapimod (R-1503, Ro4402257)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
作用于p38α和p38β酶活性,IC50分别为0.014和0.48 μM。
Pamapimod(R-1503,Ro4402257)是一种p38 MAPK抑制剂。
P38α是一种蛋白激酶,调节炎症细胞因子的表达,研究表明在诸如类风湿性关节炎和系统性红斑狼疮的疾病发病机制中具有关键作用。
体外:Pamapimod可以抑制p38alpha和p38beta酶活性,对p38delta或p38gamma无活性。对350个激酶进行分析时,pamapimod仅结合4种激酶。此外,研究发现pamapimod抑制p38,但未检测到JNK抑制。 Pamapimod还抑制LPS刺激的单核细胞TNFα产生以及IL-1β产生。此外,在啮齿动物血浆中,pamapimod还能够抑制LPS和TNFα刺激的TNFα和IL-6产生[1]。
体内:在鼠胶原诱导的关节炎中,50 mg / kg或更大剂量的Pamapimod能够减少炎症和骨丢失的临床症状。此外,Pamapimod剂量依赖性地增加痛觉过敏大鼠模型中的耐受压力,表明p38在与炎症相关的疼痛中起关键作用。此外,pamapimod类似物在狼疮易发MRL / lpr小鼠中具有相同的效力和选择性[1]。
临床试验:到目前为止,Pamapimod仍处于临床前研究阶段。
参考文献:
[1] Hill, R. J. et al. Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity. The Journal of pharmacology and experimental therapeutics 327, 610-619, doi:10.1124/jpet.108.139006 (2008).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 406.38 |
Cas No. | 449811-01-2 |
Formula | C19H20F2N4O4 |
Solubility | Soluble in DMSO |
Chemical Name | 6-(2,4-difluorophenoxy)-2-((1,5-dihydroxypentan-3-yl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |