产品说明书

C-021

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Chemical Structure| 864289-85-0 同义名 : -
CAS号 : 864289-85-0
货号 : A1216866
分子式 : C27H41N5O2
纯度 : 99%+
分子量 : 467.647
MDL号 : MFCD18661383
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(106.92 mM)，配合低频超声，并水浴加热至45℃助溶，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: 50 mg/mL(106.92 mM)，配合低频超声，并水浴加热至45℃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 C-021 is a potent CCR4 antagonist. C-021 effectively inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM[1].The in vitro oxidative metabolic stability value, i.e., the intrinsic clearance value (CLint) of C-021 was derived to be 17,377 mL/h/kg as assessed by measuring the rate of consumption of the drug in human liver microsomes (HML) [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.69mL

2.14mL

1.07mL

21.38mL

4.28mL

2.14mL
参考文献

[1]Yokoyama K, et al. Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem. 2009 Jan 1;17(1):64-73.

[2]Matthew McMillin, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121.