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C-021 2HCl

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Chemical Structure| 1784252-84-1 同义名 : C-021 dihydrochloride
CAS号 : 1784252-84-1
货号 : A936971
分子式 : C27H43Cl2N5O2
纯度 : 99%+
分子量 : 540.569
MDL号 : MFCD16618393
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 C-021 2HCl is a potent CCR4 antagonist. C-021 2HCl effectively inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. C-021 2HCl 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 of C-021 2HCl, i.e., the intrinsic clearance value (CLint), was assessed by measuring the rate of consumption of the drug in human liver microsomes (HML), yielding an in vitro oxidative metabolic stability value for C-021 2HCl of 17,377 mL/h/kg [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.25mL

1.85mL

0.92mL

18.50mL

3.70mL

1.85mL
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.