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PF-3644022 98%

PF 3644022

源葉(MedMol)
S89175
1276121-88-0
C21H18N4OS
374.46
品牌 貨號(hào) 產(chǎn)品規(guī)格 價(jià)格(RMB) 庫(kù)存（上海） 北京 武漢 南京 購(gòu)買數(shù)量
源葉(MedMol) S89175-5mg 98% ￥510.00元 5 - - -
源葉(MedMol) S89175-10mg 98% ￥950.00元 6 - - -
源葉(MedMol) S89175-25mg 98% ￥1640.00元 6 - - -
源葉(MedMol) S89175-100mg 98% ￥3600.00元 預(yù)計(jì)交期：2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect
產(chǎn)品描述： PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect
靶點(diǎn)： IC50: 5.2 nM (MK2), 5.0 nM (PRAK) and 53 nM (MK3).Ki: 3 nM (MK2);p38MAPK;?SerineProtease;?MAPK
體外研究：
The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2.
In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity.
體內(nèi)研究：
PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED50 value of 20 mg/kg. Animal Model: Female Lewis rats (125-140 g) injected with streptococcal cell wall Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg Administration: Oral gavage; twice a day; for 12 days Result: Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.
參考文獻(xiàn)：
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.
溶解性： Soluble  in  DMSO
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 2.671 ml 13.353 ml 26.705 ml
5 mM 0.534 ml 2.671 ml 5.341 ml
10 mM 0.267 ml 1.335 ml 2.671 ml
50 mM 0.053 ml 0.267 ml 0.534 ml
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