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PF-184
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-184图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PF-184 是一种有效的、选择性的IKK-2抑制剂 (IC50: 37 nM),选择性优于 rhIKK-1、IKKi, 及 30 多种酪氨酸和丝氨酸/苏氨酸激酶。PF-184 可用于炎症研究,如哮喘和慢性阻塞性肺疾病。
生物活性

PF-184 is a potent and selectiveIKK-2inhibitor (IC50: 37 nM) over rhIKK-1, IKKi, and more than 30 tyrosine and serine/threonine kinases. PF-184 can be used in the research of inflammation, such as asthma and chronic obstructive pulmonary disease[1].

IC50& Target[1]

IKK-2

37 nM (IC50)

体外研究
(In Vitro)

PF-184 (0.7 nM-10 μM, 1 h) displays inhibitory activity after successive washes of LPS-stimulated PBMC kinase activation[1].
PF-184 (1 h) broadly inhibits IKK-2-dependent inflammatory products in human disease-relevant cells (such as PBMC, neutrophils, airway epithelial cells, and airway endothelial cells), with IC50values ranging from 8 nM to 343 nM[1].
PF-184 (2 nM-10 μM, 1 h) inhibits IL-1β-induced TNF-α in a concentration-dependent manner in PBMCs[1].

体内研究
(In Vivo)

PF-184 (Intratracheal administration, 0.3-2.5 mg/mL, 100 μL) dose-dependently inhibits neutrophil infiltration and BAL cell cytokine production in rat airway inflammation model[1].
PF-184 (i.v. 2 mg/kg or p.o. 5 mg/kg, rats) shows a T1/2(i.v.) value of 1 h, low oral bioavailability (5%), and high i.v. clearance (59 mL/min/kg)[1].

Animal Model:Rat airway model of neutrophilia[1]
Dosage:0.3-2.5 mg/mL, 100 μL
Administration:Intratracheal administration
Result:Suppressed neutrophil infiltration with an EC50value of 1 mg/mL.
Suppressed BAL fluid TNF-α and PGE2levels, and inhibited p65 translocation.
分子量

619.09

Formula

C32H32ClFN6O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.