BMS-582949
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.
IC50为13 nM。
BMS-582949是一种p38 MAPK抑制剂。
p38R MAP激酶在调节多种炎症细胞因子(如肿瘤坏死因子α和白细胞介素-1β)的生物合成中起关键作用。因此,p38R抑制剂被认为是治疗炎症性疾病的有希望的疗法。
体外:研究发现,BMS-582949对p38 MAPK的选择性超过Jnk2(一种参与炎症的MAP激酶)450倍,比Raf高190倍。此外,通过X射线晶体学分析进一步证明了BMS-582949与p38R的结合模式 [1]。
体内:在假性建立的大鼠佐剂关节炎模型中,剂量为10和100 mg / kg的BMS-582949每日一次给药显示出爪肿胀剂量依赖性的减少。此外,1和5 mg/kg剂量的BMS-582949每日两次给药表现出功效改善,导致足部肿胀的极大减少。此外,低至0.3mg / kg剂量的BMS-582949每日两次给药,也观察到爪肿胀的统计学显著减少[1]。
临床试验:多中心FDG-PET试验显示,在稳定的动脉粥样硬化中,与安慰剂相比,用BMS-582949治疗12周不能减少动脉炎症或hs-CRP,而强化他汀类药物治疗可显著减少动脉炎症[ 2]。
参考文献:
[1]. Liu C, et al. Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl- N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. J Med Chem. 2010 Sep 23;53(18):6629-39.
[2]. Emami H, et al. The effect of BMS-582949, a P38 mitogen-activated protein kinase (P38 MAPK) inhibitor on arterial inflammation: a multicenter FDG-PET trial. Atherosclerosis. 2015 Jun;240(2):490-6.
Storage | Store at -20°C |
M.Wt | 406.48 |
Cas No. | 623152-17-0 |
Formula | C22H26N6O2 |
Solubility | Soluble in DMSO |
Chemical Name | 4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide |
SDF | Download SDF |
Canonical SMILES | O=C(C1=CN2N=CN=C(NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C)NCCC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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