Albany Molecular Research, Inc.
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Metabolism Screening Technologies ;vi Project g o a l : To prioritize leads from several related chemical series, each possessing comparable biological activity. Details: Several series of lead compounds had comparable biological activity. The customer sought to prioritize and develop analogs based upon favorable metabolic characteristics, including half-life. O u t c o m e : AMRI's scientists delivered the following results within two weeks: • Ranked the in vitro metabolic stability of each series and derivatives relative to others. • Identified structural features within the classes consistent with improved metabolic stability, and reported these to the medicinal chemists for further analog design. • Identified the primary human metabolic enzyme isoform involved in the metabolism of the lead series, as well as the identity of the major metabolites formed.
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21 Corporate Circle, P.O. Box 15098 Albany, New York 12212-5098 Phone:518-464-0279 Fax:518-464-0289
[email protected] www.albmolecular.com
AMRI now offers in vitro metabolic tests to support lead optimization. • Metabolic Stability Assays • Metabolic Profiling Assays • Metabolite Production • CYP450 Isoform Analysis
• Identified the mouse as an appropriate animal model system that most closely represented the human metabolic pattern for this class of compounds.
• CYP450 Inhibition Assays
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• Identified that selected derivatives of the lead series did not significantly inhibit any of the major human liver cytochrome P450 enzymes. Follow-up: Produced 10 mg of two human metabolites of interest within three weeks for further evaluation.
AMRI'S Fine Chemicals Catalog OCH 3
OH
NH2
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2HCI ChLO
N
K ^
NHBoc NHo
HO' Both enantiomers available
H,C
CT
T>H
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N
NH,
BocHN
NH2
NH,
CP Both enantiomers available
Both enantiomers available
Many phenylalanine derivatives
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Albany Molecular Research. Inc.®
21 Corporate Circle, P.O. Box 15098 • Albany, New York 12212-5098 Phone:877-388-4675 x5151 • Fax:315-458-9293 •
[email protected] • www.albmolecular.com
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