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Maraviroc Chemical Structure
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Biological Activity
A selective CCR5 (HIV-1 receptor, belongs to the G protein-coupled receptor superfamily) antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. CCR5 is an especially attractive target, since the natural genetic absence of surface-expressed CCR5 in 32 homozygous genotype populations has little apparent impact on their immune status or general health. Furthermore, this population is highly protected against HIV-1 infection[1] , and the reduced cell surface expression of CCR5 in CCR5 32 heterozygotes is associated with a slower rate of disease progression.
Maraviroc was active (IC90) at low nanomolar concentrations against HIV-1 Ba-L (alab-adapted R5 strain) when measured in a 5-day antiviral assay using either isolated multiple (pooled) donor PBMC (IC90, 3.1 nM; 95% CI, 2.0 to 4.9 nM),single-donor PBMC (IC90, 1.8 nM; 95%, CI 1.2 to 2.6 nM) or PM-1 cells (IC90, 1.1 nM; 95% CI, 0.74 to 1.7 nM).
Maraviroc inhibited MIP-1 (IC50, 3.3 nM) and RANTES (IC50, 5.2nM) binding to cell membrane preparations of CCR5-expressing HEK-293. [3]
References on Maraviroc
- [] Natyre 20 JUNE 19996;381:667-673
- [] J.Leukoc. Rio!. 1996;60: 147-152
- [] ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 2005;49:4721–4732
Chemical Information
| Molecular Weight (WM): | 513.67 |
|---|---|
| Formula: | C29H41F2N5O |
| CAS No.: | 376348-65-1 |
| Synonyms: |
UK-427857, Celsentri
|
| Dissolve in (25°C): | DMSO ≥103mg/mL |
| Water <1mg/mL | |
| Ethanol ≥103mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Analysis of receptor mechanisms mediating the induction of MMP-9 expression in THP-1 cells by AFP. Maraviroc, an inhibitor of chemokine receptor CCR5, was added to the cells in the indicated concentrations 1 hour before addition of 50 μg/ml AFP (■) or 150 ng/ml RANTES (♦). After 24 hours of cell stimulation, conditioned media were collected and analyzed for MMP-9 activity by the method of zymography
Analysis of receptor mechanisms mediating the induction of MMP-9 expression in THP-1 cells by AFP. Maraviroc, an inhibitor of chemokine receptor CCR5, was added to the cells in the indicated concentrations 1 hour before addition of 50 μg/ml AFP (■) or 150 ng/ml RANTES (♦). After 24 hours of cell stimulation, conditioned media were collected and analyzed for MMP-9 activity by the method of zymography
Data independently produced by Dr Mikhail Menshikov of Cardiology Research Center Maraviroc purchased from Selleck
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Analysis of receptor mechanisms mediating the induction of MMP-9 expression in THP-1 cells by AFP. Maraviroc, an inhibitor of chemokine receptor CCR5, was added to the cells in the indicated concentrations 1 hour before addition of 50 μg/ml AFP (■) or 150 ng/ml RANTES (♦). After 24 hours of cell stimulation, conditioned media were collected and analyzed for MMP-9 activity by the method of zymography |
Data independently produced by Dr Mikhail Menshikov of Cardiology Research Center
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