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Cat. No. : | HY-100212 |
M.Wt: | 575.72 |
Formula: | C32H37N3O5S |
Purity: | >98 % |
Solubility: | 10 mM in DMSO |
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[1][2].
IC50 & Target:IC50: 44 nM [HIV-1LAI (SI)], 24 nM [HIV-1Ba-L (SI)], 35 nM [HIV-1LAI (NSI)], 47 nM [HIV-2EHO (SI)][1]
Ki:0.33 nM (HIV-1 protease)[2]
In Vitro: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[1].
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[2].
In Vivo:JE-2147 exhibits good oral bioavailability and plasma pharmacokinetic profiles in dogs and rats[2].
Pharmacokinetic Parameters of JE-2147 in beagle dogs and male Sprague-Dawley rats[2].
Sprague-Dawley rats | Beagle dogs | ||||
i.v., 10 mg/kg | i.d., 10 mg/kg | i.v., 25 mg/kg | p.o.(fed), 25 mg/kg | p.o.(fasted), 25 mg/kg | |
t1/2β (min) | 93 | / | 94 | / | / |
Cmax (μM) | / | 0.70 ± 0.20 | / | 4.02 ± 0.72 | 5.30 ± 1.13 |
Tmax (min) | / | 60 | / | 90 | 60 |
F (%) | / | 41.6 ± 10.7 | / | 32.6 ± 0.06 | 37.1 ± 0.08 |
CL (L/h/kg) | / | / | 0.88 ± 0.09 | / | / |
Vd, ss (L/kg) | / | / | 1.58 | / | / |
AUC0-24 (μM·min) | / | / | / | 1009 | 1149 |
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