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Balicatib

Cat. No. M2600

Balicatib Structure

Synonym: AAE-581

Size Price Availability Quantity
5mg USD 110 In stock
10mg USD 150 In stock
50mg USD 445 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Balicatib is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S. Balicatib is the most advanced of them passed Phase II clinical trials in 2005.

Protocol
Cell Experiment
Cell lines Hep G2 and SMMC-7721 cells
Preparation method Cell viability assay.
The 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay was used to measure drug sensitivity. Briefly, Hep G2 and SMMC-7721 cells were seeded into 96-well plates (Corning, USA) at a density of 5 × 103 cells per well, incubated overnight, and then treated with various concentrations (0, 10, 20, 40, and 80 μmol/L) of baicalin for 24, 48, and 72 h. Thereafter, 20 μl of MTT solution (5 mg/mL; Sigma-Aldrich, St. Louis, MO, USA) was added to each well, and the plates were incubated at 37°C for 4 h. The formed formazan crystals were dissolved in 100 μl of DMSO after removal of the supernatant. The optical density (OD) was recorded at 490 nm using a microplate reader (Bio-Tek, Winooski, VT, USA). The percentage of cell viability was calculated as: (OD of baicalin-treated group/OD of control group) × 100%.
Concentrations 0, 10, 20, 40, and 80 μmol/L
Incubation time 24, 48 and 72 h
Animal Experiment
Animal models Six-week old athymic nude mice bearing Hep G2 cells xenograft model
Formulation 10% DMSO and 90% propylene glycol
Dosages 50 mg/kg and 100 mg/kg daily for 3 weeks
Administration i.p.
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 411.54
Formula C23H33N5O2
CAS Number 354813-19-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

Baicalin induces apoptosis in hepatic cancer cells in vitro and suppresses tumor growth in vivo.
Yu Y, et al. Int J Clin Exp Med. 2015 Jun 15;8(6):8958-67. PMID: 26309548.

Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
Falgueyret JP,et al. J Med Chem. 2005 Dec 1;48(24):7535-43. PMID: 16302795.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Balicatib, AAE-581 supplier, Cathepsin, inhibitors

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