• All
  • Primary Antibodies
  • Conjugated Antibodies for IF
  • Conjugated Antibodies for FC
  • Secondary Antibodies
  • Antibody Labeling KitsNew
  • ELISA Kits
  • IHC Kits
  • Magnetic Cell Separation Kits
  • Cytokines & Growth Factors
  • Neutralizing/activating Antibodies
  • Nanobody-based Reagents
  • Accessory Products and Kits
  • Fusion Proteins
×
×
Host
0
Species Reactivity
0
Species Reactivity
0
Conjugate
0
Conjugate
0
Compatible Species
0
Conjugate
0

PF-3644022

CAS号

1276121-88-0

分子式

C21H18N4OS

主要靶点

Serine Protease|p38 MAPK|MAPK

仅限科研使用

Cat No : CM06684

Print datasheet

Synonyms

Anti-inflammatory|IL-6|inhibit|efficacious|PRAK|PF3644022|PF-3644022|PF 3644022|orally|p38MAPK|p38 MAPK|monocytic|MK2|MK3|Mitogen-activated protein kinase activated protein kinase 2|MAP kinase activated protein kinase 2|MAPK activated protein kinase 2|MAPKAP kinase 2|MAPKAPK2 (MK2)|lipopolysaccharide|Inhibitor|TNFα|safety|SerineProtease|Serine Protease

验证数据展示

  • CAS No.: 1276121-88-0

    PF-3644022
    CAS#: 1276121-88-0

产品信息

CAS号 1276121-88-0
分子式 C21H18N4OS
主要靶点 Serine Protease|p38 MAPK|MAPK
主要通路 MAPK 信号通路|蛋白酶体|MAPK 信号通路
分子量 374.46
纯度 98.13%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Anti-inflammatory|IL-6|inhibit|efficacious|PRAK|PF3644022|PF-3644022|PF 3644022|orally|p38MAPK|p38 MAPK|monocytic|MK2|MK3|Mitogen-activated protein kinase activated protein kinase 2|MAP kinase activated protein kinase 2|MAPK activated protein kinase 2|MAPKAP kinase 2|MAPKAPK2 (MK2)|lipopolysaccharide|Inhibitor|TNFα|safety|SerineProtease|Serine Protease

靶点活性

PRAK:5.0 nM|MK2:(ki)3 nM|MK2:5.2 nM|MK3:53 nM

体内活性

PF-3644022（3-100 mg/kg；口服灌胃；每天两次；持续12天；Lewis大鼠）治疗显示出剂量依赖性地抑制慢性爪子肿胀。在口服给药12天后的第21天测量得ED50值为20 mg/kg[1]。

体外活性

PF-3644022在人类U937单核细胞系或周边血单核细胞中，有效抑制TNFα的产生，活性类似（IC50为160nM）。PF-3644022在LPS激活的人全血中阻断TNFα和IL-6的产生（IC50分别为1.6和10.3μM）。对其他MAPKAP激酶家族成员的抑制活性也进行了评估。除了对MNK2的IC50为148nM，PF-3644022对其他家族成员几乎没有抑制作用，显示出至少数百倍的选择性优于MK2[1]。

溶解度

DMSO:41.67 mg/mL (111.28 mM)

参考文献

1.Mourey RJ, et al. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2