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`CT@
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`Cellagen Technology, 2013
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`Product Specification Sheet
`
`Product Name:
`
`VX-478 (Am prenavir)
`
`Catalog Number:
`
`C8947
`
`Technical information:
`
`C25H35N3O6S
`161814—49—9
`
`505.63
`
`> 98%
`
`White solid
`
`Soluble in DMSO up to 30 mM
`
`(Amprenavir)
`
`Chemical Formula:
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`CAS #:
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`Molecular Weight:
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`Purity:
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`Appearance:
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`Solubility:
`Chemical Name:
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`Storage:
`Shelf Life:
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`Handling:
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`Biological Activity:
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`(3S)-oxolan-3-yl N-[(2S,3R)-3-hydroxy-4-[N-(2-methylpropy|)(4-aminobenzene)su|fonamido]-1-
`phenylbutan-2-y|]carbamate
`Store solid powder at 4°C desiccated; Store DMSO solution at -20°C.
`In the unopened package, powder is stable for 1 year and DMSO solution is stable for 6 months
`under proper storage condition.
`
`To make 10 mM stock solution, add 0.198mL of DMSO for each mg of VX-478 (Amprenavir).
`
`For DMSO solution, briefly spin the vial at 500 rpm in a 50 mL conical tube to ensure maximum
`sample recovery.
`
`Amprenavir (Agenerase, VX-478), is an orally-available, sulfonamide-based inhibitor of HIV-1, with
`relatively weak potency towards HIV-2, at IC50 values of 0.6 and 19 nM, respectively. [1] Similar to
`other HIV-1 protease inhibitors, Amprenavir binds to the active site of HIV-1 and inhibits the
`processing of the gag and gag-pol polyprotein precursors. The drug concentration of Amprenavir
`required to reduce viral production by 50% (IC50) against HIV-1 strain IIIB was 0.08 uM in acutely
`infected cells and 0.41 uM in chronically infected cells. Using a different cell line derived from a
`human T-cell lymphoma, the IC90 of Amprenavir against HIV-1 strain IIIB was 0.079 uM. [1]
`
`Human dose-escalation studies showed that Amprenavir was well tolerated at single doses up to
`1200 mg with minimal effect on absorption by food administration, unlike with other protease
`inhibitors such as indinavir, nelfinavir, and saquinavir. [2]
`
`Reference: 1-
`
`Fung et al., Amprenavir: a new human immunodeficiency virus type 1 protease inhibitor. Clin. Therapeutics,
`2000, 22(5), 549-572. Pubmed ID: 10868554
`. Sadler et al., Safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus (HIV)
`type 1 protease inhibitor, following oral administration of single doses to H|V—infected adults. Antimicrob.
`Angets. Chemother. 1999, 43(7), 1686-1692. Pubmed ID: 10390223
`
`To reorder:
`
`htt
`
`2 www.cella entech.com VX—478—Am renavir
`
`For Technical Support:
`
`technical@cellagentech.com
`
`Chemicals are sold for research use only, not for clinical or diagnostic use.
`
`Cellagen Technology | 5940 Pacific Mesa Court, Suite 206, San Diego, CA 92121, USA
`www.ce||agentech.com | Phone: 1.858.633.8197, 1.855.ce||agen (To||—free) | Fax: 1.858.228.9964
`
`Janssen Ex. 2033
`
`Lupin Ltd. v. Janssen Sciences Ireland UC
`|PR2015-01030
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