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Submit ReviewDarunavir
Description: Highly potent HIV protease inhibitor
Chemical Name: (3R,3aS,6aR)-Hexahydrofuro[2,3-b]furan-3-yl N-[(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamate
Purity: ≥98% (HPLC)
Biological Activity for Darunavir
Darunavir is a highly potent HIV protease inhibitor (IC50 = 3 - 6 nM, depending on laboratory HIV-1 strain). Displays activity in cells infected with clinical HIV-1 strains shown to have resistance to other protease inhibitors.
Tocris products are for biomedical research use only. They are not intended for human or veterinary use.
Compound Libraries for Darunavir
Darunavir is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Darunavir
| M. Wt | 547.66 |
| Formula | C27H37N3O7S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 206361-99-1 |
| PubChem ID | 213039 |
| InChI Key | CJBJHOAVZSMMDJ-HEXNFIEUSA-N |
| Smiles | [H][C@@]12CCO[C@@]1(OC[C@@H]2OC(N[C@H]([C@@H](CN(S(=O)(C3=CC=C(C=C3)N)=O)CC(C)C)O)CC4=CC=CC=C4)=O)[H] |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Darunavir
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.77 | 100 |
Preparing Stock Solutions for Darunavir
The following data is based on the product molecular weight 547.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.83 mL | 9.13 mL | 18.26 mL |
| 5 mM | 0.37 mL | 1.83 mL | 3.65 mL |
| 10 mM | 0.18 mL | 0.91 mL | 1.83 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets for Darunavir
References for Darunavir
References are publications that support the biological activity of the product.
Ghosh et al (1998) Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere. Bioorg.Med.Chem.Lett. 8 687 PMID: 9871583
Koh et al (2003) Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob.Agents Chemother. 47 3123 PMID: 14506019
If you know of a relevant reference for Darunavir, please let us know.
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Citations for Darunavir
Citations are publications that use Tocris products.
Currently there are no citations for Darunavir. Do you know of a great paper that uses Darunavir from Tocris? Please let us know.
Reviews for Darunavir
Average Rating: 5 (Based on 1 Review.)
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Interaction of darunavir with this stable portion of the protease.
By
Anonymous on 12/01/2019
Species: Human
Interaction of darunavir was studied with the stable portion of the protease. It was an attempt to finally identify interactions with HIV-1 protease and to be more resistant against HIV-1 protease mutations.
