Product Information Novel Kinase Inhibitors

for cell signaling & oncology research

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Technical Data:
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Formula: C32H44F3N5O7 enquiry@selleckchem.com
N
Solubility: DMSO N N
Purity: 99%
CF 3
Tech Support
N N
tech@selleckchem.com
Storage: at -20℃ 2 years O
C 4H 6O 5
(chemistry support)
CAS No.: 541503-81-5 Synonyms: SCH417690, SCH-D techbio@selleckchem.com
(bio support)

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Biological Activity
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In order to determine if vicriviroc 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 to inhibit
chemokine-mediated migration of a mouse Ba/F3 cell line stably expressing recombinant human
CCR5. In this assay,vicriviroc showed equally potent inhibition of the chemotactic response to MIP-1
with IC50 values below 1 nM. The ability of vicriviroc to inhibit intracellular calcium release
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induced by receptor stimulation was also assessed. A assay utilized to demonstrate the ability of
vicriviroc to inhibit CCR5 receptor signaling was a GTPS exchange assay. GTPS binding induced
by RANTES. vicriviroc potently inhibited RANTES-induced signaling with mean IC50s of
4.2 nM. [1]
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[1] Julie M. Strizki et al. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9
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