产品说明书

PF-4136309

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Chemical Structure| 1341224-83-6 同义名 : INCB8761
CAS号 : 1341224-83-6
货号 : A733437
分子式 : C29H31F3N6O3
纯度 : 99%+
分子量 : 568.59
MDL号 : MFCD22124474
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(61.56 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(175.87 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
描述 PF-4136309 exhibits potent human chemotaxis activity (IC50=3.9 nM) and effectiveness in a whole blood assay (IC50=19 nM), with IC50 values of 16 nM and 2.8 nM in mouse and rat chemotaxis assays, respectively. It strongly inhibits CCR2-mediated signaling events, such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation, with IC50 values of 3.3 nM and 0.5 nM, respectively. In hERG patch clamp assays, PF-4136309 inhibits the hERG potassium current with an IC50 of 20 μM. PF-4136309 does not inhibit cytochrome P450 (CYP), with IC50 values of >30 μM against major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4, and is not a CYP inducer at concentrations up to 30 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.79mL

1.76mL

0.88mL

17.59mL

3.52mL

1.76mL
参考文献

[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.