产品
编 号：F214408
分子式：C27H43Cl2N5O2
分子量：540.57
分子式：C27H43Cl2N5O2
分子量：540.57
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1784252-84-1
产品详情
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 IC50s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM.
体内研究：
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.Animal Model:Male C57Bl/6 mice (20-25 g) with acute liver failure
Dosage:1 mg/kg
Administration:i.p.; daily; for 3 days
Result:Significantly less microgliosis, and significantly reduced the pERK1/2 to tERK1/2 ratio.
体外研究：
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.
C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM.
体内研究：
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.Animal Model:Male C57Bl/6 mice (20-25 g) with acute liver failure
Dosage:1 mg/kg
Administration:i.p.; daily; for 3 days
Result:Significantly less microgliosis, and significantly reduced the pERK1/2 to tERK1/2 ratio.
体外研究：
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.
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