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INCB8761(PF-4136309)
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。
INCB8761(PF-4136309)图片
CAS NO:1341224-83-6
包装:5mg
市场价:1440元

产品介绍
INCB8761(PF-4136309) 是一种有效的、选择性的、可口服的 CCR2 拮抗剂,对人、小鼠和大鼠 CCR2 的 IC50 分别为 5.2 nM、17 nM 和 13 nM。
Cas No.1341224-83-6
别名INCB8761;PF-4136309;PF4136309;PF 4136309;INCB-8761
化学名N-(2-(3-((4-hydroxy-4-(5-(pyrimidin-2-yl)pyridin-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide
Canonical SMILESO=C(CNC(C1=CC(C(F)(F)F)=CC=C1)=O)N(C2)CCC2NC3CCC(C4=NC=C(C5=NC=CC=N5)C=C4)(O)CC3
分子式C29H31F3N6O3
分子量568.59
溶解度DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS(pH 7.2) (1:5): 0.17 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.

PF-4136309 is potent in human chemotaxis activity (IC50=3.9 nM) and in the whole blood assay (IC50=19 nM), with IC50 of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC50 values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC50 of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC50 values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM[1].

PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (Tmax) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species[1].

References:
[1]. Xue CB, et al. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. ACS Med. Chem. Lett., 2011, 2 (12), pp 913-918.