产品描述 | LDC4297 hydrochloride is a selective inhibitor ofCDK7with anIC50value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with anEC50value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities toHerpesviridae,Adenoviridae,Poxviridae,RetroviridaeandOrthomyxoviridaewithEC50values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection[1]. LDC4297 hydrochloride (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50value of 24.5 nM[1]. LDC4297 hydrochloride (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50value of 4.5 μM[1]. LDC4297 hydrochloride (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation[1]. LDC4297 hydrochloride (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 EC50values 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[1]. Western Blot Analysis[1] Cell Line: | Primary cultures of fibroblasts derived from human (HFF) with virus infection | Concentration: | 20 μM | Incubation Time: | 12, 24, 48 and 96 hours | Result: | Showed inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and reduced Rb expression in the uninfected control cells at 24 h. |
LDC4297 hydrochloride (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses[1]. Animal Model: | CD1 mice[1] | Dosage: | 100 mg/kg | Administration: | Oral gavage; 100 mg/kg once | Result: | Showed a half-life (t1/2z) of 1.6 h, and the time to a mean peak plasma concentration of 1297.6 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%. |
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