JE-2147
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.
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- CAS No.: 186538-00-1
- Formule: C32H37N3O5S
- Masse moléculaire:575.72
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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]
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Cell Line
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Type | Value | Description | References |
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| CEM-SS | IC50 |
7 nM
Compound: 21f
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Antiviral activity was determined based on inhibition of HIV-1 IIIB induced cytopathic effects in CEM-SS cells in vitro using tetrazolium reagent.
Antiviral activity was determined based on inhibition of HIV-1 IIIB induced cytopathic effects in CEM-SS cells in vitro using tetrazolium reagent.
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[PMID: 10346931] |
| MT4 | EC50 |
0.033 μM
Compound: 1, KNI-764
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Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 19954246] |
| MT4 | EC50 |
0.06 μM
Compound: 1, KNI-764
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Antiviral activity against HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 19954246] |
| MT4 | EC50 |
0.1 μM
Compound: 1, KNI-764
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Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
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[PMID: 19954246] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle dogs and male Sprague-Dawley rats[2]
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Dosage:25 mg/kg for dogs; 10 mg/kg for rats
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Administration:i.v. and i.d. for rats; i.v. and p.o. for dogs.
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Result:Exhibited favorable pharmacokinetic properties.
Chemical Information
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CAS No. 186538-00-1
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Masse moléculaire 575.72
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Formule C32H37N3O5S
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SMILES
CC(C=CC=C1)=C1CNC([C@H]2N(CSC2(C)C)C([C@@H](O)[C@@H](NC(C3=C(C(O)=CC=C3)C)=O)CC4=CC=CC=C4)=O)=O
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Synonyms
AG1776; KNI-764
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JE-2147 Related Classifications
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