产品
编 号：F233713
分子式：C32H37N3O5S
分子量：575.72
分子式：C32H37N3O5S
分子量：575.72
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CAS No: 186538-00-1
产品详情
生物活性：
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro.
体内研究：
JE-2147 exhibits good oral bioavailability and plasma pharmacokinetic profiles in dogs and rats.Pharmacokinetic Parameters of JE-2147 in beagle dogs and male Sprague-Dawley rats.Sprague-Dawley rats Beagle dogs
i.v., 10 mg/kgi.d., 10 mg/kgi.v., 25 mg/kgp.o.(fed), 25 mg/kgp.o.(fasted), 25 mg/kg
t1/2β (min)93/94//
Cmax (μM)/0.70?±?0.20/4.02?±?0.725.30?±?1.13
Tmax (min)/60/9060
F (%)/41.6?±?10.7/32.6?±?0.0637.1?±?0.08
CL (L/h/kg)//0.88?±?0.09//
Vd, ss (L/kg)//1.58//
AUC0-24 (μM·min)///10091149
Animal Model:Beagle dogs and male Sprague-Dawley rats
Dosage:25 mg/kg for dogs; 10 mg/kg for rats
Administration:i.v. and i.d. for rats; i.v. and p.o. for dogs.
Result:Exhibited favorable pharmacokinetic properties.
体外研究：
JE-2147 (0.01-0.05 μM; 7 days; PBMC and MT-2 cells) exhibits highly potent antiviral activity against HIV-1 with IC50s of 44 nM, 24 nM, 35 nM and 47 nM for HIV-1LAI (SI), HIV-1Ba-L (SI), HIV-1LAI (NSI) and HIV-2EHO (SI), respectively.JE-2147 is effective against the replication of HIV-1 IIIB in various cells (T cell, B cell, macrophage, and PBMC) with IC50 values ranging from 31 to 160 nM and also had antiviral activity against simian immunodefidiency virus and HIV-2.
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro.
体内研究：
JE-2147 exhibits good oral bioavailability and plasma pharmacokinetic profiles in dogs and rats.Pharmacokinetic Parameters of JE-2147 in beagle dogs and male Sprague-Dawley rats.Sprague-Dawley rats Beagle dogs
i.v., 10 mg/kgi.d., 10 mg/kgi.v., 25 mg/kgp.o.(fed), 25 mg/kgp.o.(fasted), 25 mg/kg
t1/2β (min)93/94//
Cmax (μM)/0.70?±?0.20/4.02?±?0.725.30?±?1.13
Tmax (min)/60/9060
F (%)/41.6?±?10.7/32.6?±?0.0637.1?±?0.08
CL (L/h/kg)//0.88?±?0.09//
Vd, ss (L/kg)//1.58//
AUC0-24 (μM·min)///10091149
Animal Model:Beagle dogs and male Sprague-Dawley rats
Dosage:25 mg/kg for dogs; 10 mg/kg for rats
Administration:i.v. and i.d. for rats; i.v. and p.o. for dogs.
Result:Exhibited favorable pharmacokinetic properties.
体外研究：
JE-2147 (0.01-0.05 μM; 7 days; PBMC and MT-2 cells) exhibits highly potent antiviral activity against HIV-1 with IC50s of 44 nM, 24 nM, 35 nM and 47 nM for HIV-1LAI (SI), HIV-1Ba-L (SI), HIV-1LAI (NSI) and HIV-2EHO (SI), respectively.JE-2147 is effective against the replication of HIV-1 IIIB in various cells (T cell, B cell, macrophage, and PBMC) with IC50 values ranging from 31 to 160 nM and also had antiviral activity against simian immunodefidiency virus and HIV-2.
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