GLPBio

PNU-103017

Catalog No.: GC32327Purity:>98%
COASDSData Sheet
PNU-103017 is an HIV protease inhibitor.

Products are for research use only. Not for human use. We do not sell to patients.

PNU-103017
Cas No.: 166335-18-8
1mgIn Stock
$1,553.00
1
5mgIn Stock
$2,486.00
1
10mgIn Stock
$3,979.00
1
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Citations

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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    35, 97–116 (2025)
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Description

PNU-103017 is an HIV protease inhibitor.

PNU-103017 is a selective HIV aspartyl protease inhibitor under evaluation as a potential oral treatment of Acquired Immunodeficiency Diseases. PNU-103017 is a racemic mixture of two enantiomers, designated PNU-103264 (R-) and PNU-103265 (S-). The Cmax (P≤0.0349), Cmin (P≤0.0168), and Cav (P≤0.0118) are significantly higher for the (R)- than the (S)-enantiomer, showing enantioselective pharmacokinetics of PNU-103017 in the dog[1].

[1]. Williams MG, et al. Stereospecific determination of an HIV aspartyl protease inhibitor, PNU-103017, in rat, dog and human plasma using a Pirkle-concept high-performance liquid chromatographic column.

Protocol

Animal experiment:

Rats and dogs are used in this study. In preclinical toxicology studies, dogs (three per gender per dose) receive 50, 100, 200, or 250 mg/kg/day, and rats (three per gender per dose) receive 80, 240, or 720 mg/kg/day PNU-103017 in a 0.5 N sodium hydroxide aqueous solution orally, twice daily, 8 and 16 h apart, respectively, for 14 days. Sequential blood specimens are collected at 0 (prior to the first daily dosing), 1, 2, 4, 8 (prior to the second daily dosing), 9, 10, 12, 16 (for dog only), and 24 h after the first daily dosing on treatment days 1, 8, and 14 for the dog and rat studies. The samples are placed into heparinized tubes, and the plasma is separated by centrifugation and stored at or below -10°C until analysis[1].

References:

[1]. Williams MG, et al. Stereospecific determination of an HIV aspartyl protease inhibitor, PNU-103017, in rat, dog and human plasma using a Pirkle-concept high-performance liquid chromatographic column.

Chemical Properties

CAS No.
166335-18-8
SMILES
O=S(C1=CC=C(C#N)C=C1)(NC2=CC=CC(C(C3CC3)C4=C(O)C(CCCCCC5)=C5OC4=O)=C2)=O
Molecular Formula
C28H28N2O5S
Molecular Weight
504.6
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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