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Vicriviroc Malate Chemical Structure
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Biological Activity
In order to determine if vicriviroc malate is a receptor agonist or antagonist, three functional assays were employed to measure the ability of the compound to block b-chemokine signaling in CCR5-expressing cells.A chemotaxis assay was first employed to determine the ability of vicriviroc malate to inhibit chemokine-mediated migration of a mouse Ba/F3 cell line stably expressing recombinant human CCR5. In this assay, vicriviroc malate showed equally potent inhibition of the chemotactic response to MIP-1 with IC50 values below 1 nM. The ability of vicriviroc malate to inhibit intracellular calcium release induced by receptor stimulation was also assessed. A assay utilized to demonstrate the ability of vicriviroc malate to inhibit CCR5 receptor signaling was a GTPS exchange assay. GTPS binding induced by RANTES. vicriviroc malate potently inhibited RANTES-induced signaling with mean IC50s of 4.2 nM. [1] Vicriviroc Malate is highly water-soluble and demonstrates oral bioavailability of >89% in rats and monkeys. The compound is modestly human plasma protein-bound (≈84%) and widely distributed in the extra vascular space.Absorption and exposure in humans are linear and doseproportional, with a terminal phase half-life >24 hours supportive of once daily dosing. Variability in absorption is modest (20–40%). [2] Vicriviroc Malate is NOT A p-glycoprotein Substrate In Vitro. [3]
References on Vicriviroc Malate
- [] ANTIMICROBIAL AGENTS AND CHEMOTHERAPY Dec. 2005;49:4911–4919
- [] Retrovirology 2005;2(Suppl 1):S12
- [] Retrovirology 2005;2(Suppl 1):P158
Chemical Information
| Molecular Weight (WM): | 667.72 |
|---|---|
| Formula: | C28H38F3N5O2.C4H6O5 |
| CAS No.: | 541503-81-5 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥134mg/mL |
| Water ≥38mg/mL | |
| Ethanol ≥134mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Selleck's high quality products have been used in several published research findings, including the following:
Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro
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PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
Data from [J Antimicrob Chemother 2011.January;66:802-812] Vicriviroc Malate purchased from Selleck
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mdr1a/b and ABCB1 inhibition measured by calcein assay. Concentration-dependent effects of elvitegravir and vicriviroc on calcein accumulation in P388/dx cells (a) and L-MDR1 cells (b). Each curve depicts one representative experiment of a series of three or four. Data are expressed as means+SEM.
mdr1a/b and ABCB1 inhibition measured by calcein assay. Concentration-dependent effects of elvitegravir and vicriviroc on calcein accumulation in P388/dx cells (a) and L-MDR1 cells (b). Each curve depicts one representative experiment of a series of three or four. Data are expressed as means+SEM.
Data from [J Antimicrob Chemother 2011.January;66:802-812] Vicriviroc Malate purchased from Selleck
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Effect of antiretrovirals and positive control rifampicin (at 10 mmol/L) on ABCB1 function in LS180 cells after 3 and 7 days (d) of treatment. ABCB1 function was normalized to the medium control. Data are expressed as means+SEM for n¼4. **P,0.01.
Effect of antiretrovirals and positive control rifampicin (at 10 mmol/L) on ABCB1 function in LS180 cells after 3 and 7 days (d) of treatment. ABCB1 function was normalized to the medium control. Data are expressed as means+SEM for n¼4. **P,0.01.
Data from [J Antimicrob Chemother 2011.January;66:802-812] Vicriviroc Malate purchased from Selleck
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PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
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Data from [J Antimicrob Chemother 2011.January;66:802-812]
mdr1a/b and ABCB1 inhibition measured by calcein assay. Concentration-dependent effects of elvitegravir and vicriviroc on calcein accumulation in P388/dx cells (a) and L-MDR1 cells (b). Each curve depicts one representative experiment of a series of three or four. Data are expressed as means+SEM. |
Data from [J Antimicrob Chemother 2011.January;66:802-812]
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