JE-2147  (Synonyms: AG1776; KNI-764)

JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a K_i 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: 44 nM [HIV-1_LAI (SI)], 24 nM [HIV-1_Ba-L (SI)], 35 nM [HIV-1_LAI (NSI)], 47 nM [HIV-2_EHO (SI)]^[1]
K_i:0.33 nM (HIV-1 protease)^[2]

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-1_LAI (SI), HIV-1_Ba-L (SI), HIV-1_LAI (NSI) and HIV-2_EHO (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

575.72

C₃₂H₃₇N₃O₅S

186538-00-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yoshimura K, et al. JE-2147: a dipeptide protease inhibitor (PI) that potently inhibits multi-PI-resistant HIV-1. Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8675-80.  [Content Brief]

  [2]. Mimoto T, et al. Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine. J Med Chem. 1999 May 20;42(10):1789-802.  [Content Brief]