AEBSF HCl is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, plasmin, thrombin, and trypsin. AEBSF hydrochloride inhibits the constitutive production of A beta in five different human cell lines, both neural and nonneural. AEBSF HCl also stabilizes full-length beta APP and enhances alpha-secretion, as shown by an increase in the proteolytic derivative, alpha-APPS. AEBSF (76.8 mg/kg daily i.p.) results in prolongation of the survival of mice that have been given a lethal T. gondii infection. AEBSF also reduces airway response and underlying inflammation in cockroach allergen-induced murine model.
Front Immunol. 2023 Mar 15;14:1127552.
Giardia duodenalis-induced G0/G1 intestinal epithelial cell cycle arrest and apoptosis involve activation of endoplasmic reticulum stress in vitro
AEBSF HCl purchased from AbMole
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Source | Contraception (2011). Figure 3. AEBSF HCl |
| Method | MTT assay | |
| Cell Lines | HeLa cells | |
| Concentrations | 10, 20 mcg/mL | |
| Incubation Time | 24 h | |
| Results | Inhibitory effect of AEBSF on embryo implantation might, at least in part, result from its interference in the adhesion and invasion of blastocyst cells to maternal endometrial tissue during the implantation process. |
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Source | Contraception (2011). Figure 2. AEBSF HCl |
| Method | cell culture | |
| Cell Lines | endometrial cells | |
| Concentrations | 50 mcg/mL | |
| Incubation Time | 5 d | |
| Results | It was observed that AEBSF not only disturbed the attachment and outgrowth of mouse blastocysts on endometrial cells but also inhibited the adhesion and proliferation of HeLa cells on HUVECs |
| Cell Experiment | |
|---|---|
| Cell lines | HUVECs |
| Preparation method | When HUVECs were grown to 60%∼70% confluence, the culture medium was changed, and 150 μL new media with different concentrations of AEBSF (0, 10, 20 mcg/mL) were added to the adherent cells. After 24 h of the AEBSF treatment, 50 μL BCECF-AM- labeled HeLa cells (ATCC) were seeded onto HUVEC monolayers (105 cells/well) and co-cultured for 4 h. |
| Concentrations | 0, 10, 20 mcg/mL |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Adult Sprague–Dawley (SD) rats |
| Formulation | saline |
| Dosages | 5 or 10 mg/kg |
| Administration | i.e. |
| Molecular Weight | 239.69 |
| Formula | C8H11ClFNO2S |
| CAS Number | 30827-99-7 |
| Solubility (25°C) | Water ≥ 90 mg/mL DMSO ≥ 60 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.
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