C-021 dihydrochloride|1784252-84-1|-陌孚医药/Medlife

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C-021 dihydrochloride

目录号: PL01405

CAS No. :1784252-84-1

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中文名称	C-021 dihydrochloride
英文名称	C-021 dihydrochloride
英文别名	C 021 dihydrochloride;2-[1,4'-BIPIPERIDIN]-1'-YL-N-CYCLOHEPTYL-6,7-DIMETHOXY-4-QUINAZOLINAMINE DIHYDROCHLORIDE;C-021 dihydrochloride
Cas No.	1784252-84-1
分子式	C₂₇H₄₃Cl₂N₅O₂
分子量	540.57
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	C-021 dihydrochloride 是有效的 CC 趋化因子受体 4 (CCR4) 拮抗剂。C-021 dihydrochloride 有效抑制人和小鼠的功能趋化性，IC₅₀ 分别为 140 nM 和 39 nM。C-021 dihydrochloride 以 IC₅₀ 为 18 nM 来有效阻止人 CCL22 衍生的 [³⁵S]GTPγS 与受体结合。
生物活性	C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC 50 s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [S]GTPγS from binding to the receptor with an IC 50 of 18 nM.
性状	Solid
IC50 & Target[1][2]	CCR4
体外研究(In Vitro)	The in vitro oxidative metabolic stability of C-021 (Compound 1b) is evaluated by measuring the rate of drug consumption in human liver microsomes (HML), thus providing intrinsic clearance values (CLint). C-021 exhibits CLint value of 17,377 mL/h/kg. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	The potency of C-021 (Compound 1b) is evident after subcutaneous administration in the murine oxazolone-induced contact hypersensitivity test, a known model of acute skin inflammation. When C-021 is administered orally, however, very little inhibition is observed. C-021 (1 mg/kg; i.p.; daily; for 3 days) significantly less microgliosis in acute liver failuremice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.

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