ELND006

Stock Code: 3575842
Manufacturer Part No: SML2122-25MG
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£537.64 (exc VAT) per 25MG
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Biochem/physiol Actions


ELND006 is an allosteric γ-secretase inhibitor that selectively blocks amyloid-β (Aβ) over Notch production both in cell-free (Aβ IC50/Notch IC50 = 0.34 nM/6.6 nM) and cell-based assays (Aβ IC50/Notch IC50 = 1.3 nM/85 nM). ELND006 is orally available and blood-brain barrier-permeable (total/unbound conc in brain = 0.12 µM/1.0 nM, 0.52 µM/4.5 nM, 2.1 µM/18 nM and total/unbound conc in plasma = 0.031 µM/0.28 nM, 0.19 µM/1.7 nM, 0.90 µM/8.1 nM 3 h post 1, 3, 10 mg/kg oral dosage in rats, respectively), and shown to effectively reduce cortical Aβx-40 in mice in vivo (by 32%, 48%, and 61% 3 h post 1, 3, 10 mg/kg oral dosage).

Colourwhite to beige
ManufacturerSIGMA-ALDRICH
Storage Temp.2-8°C
SolubilityDMSO: 2 mg/mL, clear
Formpowder
Assay≥98% (HPLC)

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