1. Anti-infection
  2. HIV
  3. BMS-585248

BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile.

For research use only. We do not sell to patients.

BMS-585248 Chemical Structure

BMS-585248 Chemical Structure

CAS No. : 619331-12-3

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Description

BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile[1].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
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
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]
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: 3
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]
In Vivo

BMS-585248 (intravenous (1 mg/kg) and oral (5-200 mg/kg); once) has a good pharmacokinetic profile, with AUC values of 3220 nM·h and 8064 nM·h after IV (1 mg/kg) and oral (5 mg/kg) administration in male rats, respectively[1].

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

Animal Model: Male rats[1]
Dosage: 5, 15, and 200 mg/kg
Administration: Orally, once (Pharmacokinetic Analysis)
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
Molecular Weight

447.42

Formula

C22H18FN7O3

CAS No.
SMILES

O=C(N1CCN(C(C2=CC=CC=C2)=O)CC1)C(C3=CNC4=C3C(F)=CN=C4N5N=NC=C5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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BMS-585248 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BMS-585248
Cat. No.:
HY-13829
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