BMS-585248
BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 619331-12-3
- Fòrmula: C22H18FN7O3
- Peso molecular:447.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
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HIV-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | CC50 |
>300 μM
Compound: 12m, BMS-585428
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 23360431] |
| MT2 | EC50 |
0.8 nM
Compound: 12m, BMS-585428
|
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in absence of human serum
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in absence of human serum
|
[PMID: 23360431] |
| MT2 | EC50 |
0.87 nM
Compound: 12m, BMS-585428
|
Antiviral activity against X4-tropic HIV1 LAI infected in MT2 cells
Antiviral activity against X4-tropic HIV1 LAI infected in MT2 cells
|
[PMID: 23360431] |
| MT2 | EC50 |
1.32 nM
Compound: 12m, BMS-585428
|
Antiviral activity against X4-tropic HIV1 NL4-3 infected in MT2 cells
Antiviral activity against X4-tropic HIV1 NL4-3 infected in MT2 cells
|
[PMID: 23360431] |
| MT2 | EC50 |
2.3 nM
Compound: 12m, BMS-585428
|
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in presence of human serum
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in presence of human serum
|
[PMID: 23360431] |
| MT2 | EC50 |
5.17 nM
Compound: 12m, BMS-585428
|
Antiviral activity against X4-tropic HIV1 MN infected in MT2 cells
Antiviral activity against X4-tropic HIV1 MN infected in MT2 cells
|
[PMID: 23360431] |
| U-87MG ATCC | IC50 |
<5 nM
Compound: 29
|
Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay
Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay
|
[PMID: 18052117] |
| U-87MG ATCC | CC50 |
>40000 nM
Compound: 29
|
Cytotoxicity against human U87 cells expressing CD4 and CXCR4
Cytotoxicity against human U87 cells expressing CD4 and CXCR4
|
[PMID: 18052117] |
| U-87MG ATCC | CC50 |
>40000 nM
Compound: 3
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Cytotoxicity against human U87 cells coexpressing CD4, CxCR4 receptors after 72 hrs
Cytotoxicity against human U87 cells coexpressing CD4, CxCR4 receptors after 72 hrs
|
[PMID: 19534463] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats[1]
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Dosage:5, 15, and 200 mg/kg
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Administration:Orally, once (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of BMS-585248 in male rats[1].
PO Dose (mg/kg) 15 75 200 Cmax (μM) 6.6 8.4 11 AUCtot (μM·h) 42 115 145
Chemical Information
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No. CAS 619331-12-3
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Peso molecular 447.42
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Fòrmula C22H18FN7O3
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SMILES
O=C(N1CCN(C(C2=CC=CC=C2)=O)CC1)C(C3=CNC4=C3C(F)=CN=C4N5N=NC=C5)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)