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Cat. No. M3523
YO-01027 Structure

Dibenzazepine; DBZ

Size Price Availability Quantity
2mg USD 70  USD70 In stock
5mg USD 92  USD92 In stock
10mg USD 165  USD165 In stock
25mg USD 360  USD360 In stock
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Quality Control
Biological Activity

YO-01027 is a dipeptidic gamma-secretase inhibitor with IC50 of 2.6 and 2.9 nM for the proteolysis of APPL and Notch, respectively. YO-01027 is used as an anti-Alzheimer agent. YO-01027 directly interact with the gamma-secretase complex. Unlike other gamma-secretase inhibitors,YO-01027 targets different functional domain of the complex. YO-01027 targets the N-terminal Presenilin fragment as well as another gamma-secretase inhibitor Compound E (Cpn E), whereas DFK167 and DAPT, another two gamma-secretase inhibitors, bind to the catalytic site of the Presenilin aspartyl protease subunit and the C-terminal Presenilin fragment, respectively. In a study, YO-01027 and CpnE indicated no apparent discrimination in blocking APPL and Notch cleavages, displaying statistically equivalent IC50 values for both substrates.

Cell Experiment
Cell lines BCSC
Preparation method Resuspending cells at ≤1 × 106 in 100 μL sorting buffer (PBS containing 0.5% bovine serum albumin, 2 mM EDTA) and incubating with preconjugated primary antibodies BEREP4-FITC (1:10), CD44-APC (1:20), and CD24-PE (1:10) for 10 minutes at 4 °C. Washing the cells in PBS and centrifuged at 800 × g for 2 minutes. For analysis, cells are resuspending in 500 μL of sorting buffer and using FACSCalibur to measure fluorescence and using WinMIDI 2.8 to analyze . For sorting, cells are resuspended in 1× HBSS after incubation with the primary antibodies. Cells are sorted, with HBSS as sheath fluid, at 16 p.s.i. using FACSAria. The CD24low cell population gated by FACS is the lowest quintile of CD24-positive cells plus all the CD24-negative cells.
Concentrations 10 μM
Incubation time 3 days
Animal Experiment
Animal models C57BL/6 mice
Formulation 0, 3Injected daily intraperitoneally, 10, 30 μmol/kg
Dosages YO-01027 is suspended finely in 0.5% (w/v) hydroxypropylmethylcellulose (Methocel E4M) and 0.1% (w/v) Tween 80 in water.
Administration Injected daily intraperitoneally
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 463.48
Formula C26H23F2N3O3
CAS Number 209984-56-5
Purity 100.00%
Solubility DMSO 83 mg/mL
Storage at -20°C
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Abmole Inhibitor Catalog 2017

Keywords: YO-01027, Dibenzazepine; DBZ supplier, Gamma-secretase, inhibitors

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