1. Metabolic Enzyme/Protease
    Anti-infection
  2. HIV Protease
    HIV

PNU-103017 

Cat. No.: HY-19236
Handling Instructions

PNU-103017 is an HIV protease inhibitor.

For research use only. We do not sell to patients.

PNU-103017 Chemical Structure

PNU-103017 Chemical Structure

CAS No. : 166335-18-8

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1 mg USD 1690 Get quote
5 mg USD 2705 Get quote
10 mg USD 4328 Get quote

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PNU-103017 is an HIV protease inhibitor.

IC50 & Target

HIV protease[1]

In Vivo

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9818 mL 9.9088 mL 19.8177 mL
5 mM 0.3964 mL 1.9818 mL 3.9635 mL
10 mM 0.1982 mL 0.9909 mL 1.9818 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

504.60

Formula

C₂₈H₂₈N₂O₅S

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PNU-103017
Cat. No.:
HY-19236
Quantity:

PNU-103017

Cat. No.: HY-19236