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.
 |
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. |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 593.73 |
| Formula | C27H37N3O7S.C2H5OH |
| CAS Number | 635728-49-3 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[1] Nguyen DN, et al. Int J Pharm. The fate of ritonavir in the presence of darunavir.
| Related HIV Protease Products |
|---|
| Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2
Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 is a fluorogenic substrate of HIV-1 protease. |
| Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2
Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 is a substrato peptídico of HIV-1 protease. |
| HIV-1, HIV-2 Protease Substrate
HIV-1, HIV-2 Protease Substrate is the substrate of HIV-1, HIV-2 protease. |
| HIV Protease Substrate IV
HIV Protease Substrate IV is a substrate of HIV protease. |
| Herpes virus inhibitor 2
Herpes virus inhibitor 2 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
