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Darunavir Ethanolate

Cat. No. M3568
Darunavir Ethanolate Structure
Synonym:

TMC114

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 53.1  USD59 In stock
5mg USD 42.3  USD47 In stock
10mg USD 74.7  USD83 In stock
50mg USD 229.5  USD255 In stock
100mg USD 402.3  USD447 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

Darunavir Ethanolate is an inhibitor of HIV protease. Darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including strains from treatment-experienced patients with multiple resistance mutations to PIs.

Customer Product Validations & Biological Datas
Source AAPS PharmSciTech (2017). Figure 7.Darunavir Ethanolate
Method LC-MS method
Cell Lines Wistar rats
Concentrations 40 mg/kg
Incubation Time 0.5, 1, 2, 4, 8, and 24 h
Results The plasma concentration of darunavir in rats after oral administration of SLNs and peptide-grafted SLNs showed no significant difference (P > 0.5).
Source AAPS PharmSciTech (2017). Figure 4.Darunavir Ethanolate
Method Identification of Internalization Pathway
Cell Lines Caco-2 cell line
Concentrations
Incubation Time 0.5, 1, 2, 3, and 4 h
Results The relative uptake efficiency of darunavir in presence of endocytic inhibitors is graphically depicted in Fig. 4.
Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 593.73
Formula C27H37N3O7S.C2H5OH
CAS Number 635728-49-3
Purity >99%
Solubility DMSO ≥ 50 mg/mL
Storage at -20°C
References

The fate of ritonavir in the presence of darunavir.
Nguyen DN, et al. Int J Pharm. 2014 Nov 20;475(1-2):214-26. PMID: 25180992.

Hepatobiliary and intestinal elimination of darunavir in an integrated preclinical rat model.
Stappaerts J, et al. Xenobiotica. 2014 Jun;44(6):489-97. PMID: 24274355.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Darunavir Ethanolate, TMC114 supplier, HIV Protease, inhibitors

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