C-021 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

C-021 diHClide 是一种有效的口服生物可利用的 CCR4 拮抗剂。

C-021 dihydrochloride is a potent and orally bioavailable CCR4 antagonist with IC50 of 0.14 uM and 0.039 uM for inhibition of chemotaxis in human and mouse, respectively.

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.

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.

C021 dihydrochloride

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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1784252-84-1

540.57

C27H41N5O2.2HCl

>98% (HPLC)

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COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCC(CC3)N4CCCCC4)NC5CCCCCC5)OC.Cl.Cl

2-([1,4'-bipiperidin]-1'-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine dihydrochloride

(-20℃)

With Ice Pack

≥ 2 years