目錄:MedChemExpress LLC>>生化試劑>> CCR4-351 | MCE
CAS | 2174938-70-4 | 純度 | 98.02% |
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分子量 | 500.42 | 分子式 | C??H??Cl?N?O |
供貨周期 | 現貨 | 規格 | 10 mg |
貨號 | HY-131349 | 應用領域 | 醫療衛生,化工,生物產業,制藥 |
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CAS No. : 2174938-70-4
產品活性:CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.
研究領域:GPCR/G Protein | Immunology/Inflammation
作用靶點:CCR
In Vitro: CCR4-351 (compound 38) shows no activity in a CYP450 induction assay.
CCR4-351 inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM.
In Vivo: CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth.
CCR4-351 (0.5 mg/kg; IV) has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
CCR4-351 has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4-351 has low clearance (CL=3.7 mL/min/kg), a long terminal half-life (10.7 hr), and good bioavailability (%F = 41) in cynomolgus monkey.
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