ELND006

ELND006

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).

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575842 ELND006 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£537.64 (exc VAT) per 25MG
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3575843 ELND006 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£169.93 (exc VAT) per 5MG
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