JE-2147


CAS No. : 186538-00-1

(Synonyms: AG1776; KNI-764)

186538-00-1
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Cat. No. : HY-100212
M.Wt: 575.72
Formula: C32H37N3O5S
Purity: >98 %
Solubility: 10 mM in DMSO
Introduction of 186538-00-1 :

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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