SML2122
ELND006
≥98% (HPLC)
Synonym(s):
(R)-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline
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5 MG
$121.60
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Available to ship onApril 30, 2025Details
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5 MG
$121.60
25 MG
$203.50
About This Item
Empirical Formula (Hill Notation):
C20H14F5N3O2S
CAS Number:
Molecular Weight:
455.40
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
$121.60
List Price$128.00Save 5%Web-Only Promotion
Available to ship onApril 30, 2025Details
Recommended Products
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -125 to -140°, c = 0.5 in ethanol
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Related Categories
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).
Orally active allosteric γ-secretase inhibitor that selectively inhibits the production of amyloid-β (Aβ) over Notch with brain Aβx-40-lowering efficacy in vivo.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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Localization and Processing of the Amyloid-β Protein Precursor in Mitochondria-Associated Membranes.
Dolores Del Prete et al.
Journal of Alzheimer's disease : JAD, 55(4), 1549-1570 (2016-12-03)
Alteration of mitochondria-associated membranes (MAMs) has been proposed to contribute to the pathogenesis of Alzheimer's disease (AD). We studied herein the subcellular distribution, the processing, and the protein interactome of the amyloid-β protein precursor (AβPP) and its proteolytic products in
Xiaocong M Ye et al.
Bioorganic & medicinal chemistry letters, 23(4), 996-1000 (2013-01-15)
Structure-activity relationship (SAR) of a novel, potent and metabolically stable series of benzo [3.2.1] bicyclic sulfonamide-pyrazoles as γ-secretase inhibitors are described. Compounds that are efficacious in reducing the cortical Aβx-40 levels in FVB mice via oral dose, as well as
Inger Lauritzen et al.
Acta neuropathologica, 132(2), 257-276 (2016-05-04)
Endosomal-autophagic-lysosomal (EAL) dysfunction is an early and prominent neuropathological feature of Alzheimers's disease, yet the exact molecular mechanisms contributing to this pathology remain undefined. By combined biochemical, immunohistochemical and ultrastructural approaches, we demonstrate a link between EAL pathology and the
Inger Lauritzen et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 32(46), 16243-1655a-16243-1655a (2012-11-16)
Triple-transgenic mice (3xTgAD) overexpressing Swedish-mutated β-amyloid precursor protein (βAPP(swe)), P310L-Tau (Tau(P301L)), and physiological levels of M146V-presenilin-1 (PS1(M146V)) display extracellular amyloid-β peptides (Aβ) deposits and Tau tangles. More disputed is the observation that these mice accumulate intraneuronal Aβ that has been
Rampurna Gullapalli et al.
Drug delivery, 19(5), 239-246 (2012-06-05)
Hydrophilic, non-aqueous solvents are frequently used to solubilize poorly water soluble compounds for use in ALZET® osmotic pumps used during the discovery and preclinical stages. Though these solvents exhibit the potential to solubilize several poorly soluble compounds, the solubilized compounds
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