产品
编 号:F167838
分子式:C23H28N8O
分子量:432.52
产品类型
结构图
CAS No: 1453834-21-3
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产品详情
生物活性:
LDC4297 is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 value of 0.02-1.21 μM. LDC4297 can be used for the research of infection.
体内研究:
LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses.Animal Model:CD1 mice
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg once
Result:Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.
体外研究:
LDC4297 (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50 value of 24.5 nM.LDC4297 (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50 value of 4.5 μM.LDC4297 (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation.LDC4297 (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC50 values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively.