Direkt zum Inhalt
Merck

SML2122

Sigma-Aldrich

ELND006

≥98% (HPLC)

Synonym(e):

(R)-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline

Anmeldenzur Ansicht organisationsspezifischer und vertraglich vereinbarter Preise


About This Item

Empirische Formel (Hill-System):
C20H14F5N3O2S
CAS-Nummer:
Molekulargewicht:
455.40
MDL-Nummer:
UNSPSC-Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Optische Aktivität

[α]/D -125 to -140°, c = 0.5 in ethanol

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear

Lagertemp.

2-8°C

Biochem./physiol. Wirkung

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).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3


Hier finden Sie alle aktuellen Versionen:

Analysenzertifikate (COA)

Lot/Batch Number

Leider sind derzeit keine COAs für dieses Produkt online verfügbar.

Wenn Sie Hilfe benötigen, wenden Sie sich bitte an Kundensupport

Besitzen Sie dieses Produkt bereits?

In der Dokumentenbibliothek finden Sie die Dokumentation zu den Produkten, die Sie kürzlich erworben haben.

Die Dokumentenbibliothek aufrufen

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
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
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
Kevin Quinn et al.
Journal of pharmaceutical sciences, 101(4), 1462-1474 (2012-01-04)
ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability, suggesting it is a Biopharmaceutics Classification System Class II compound. The poor absolute

Unser Team von Wissenschaftlern verfügt über Erfahrung in allen Forschungsbereichen einschließlich Life Science, Materialwissenschaften, chemischer Synthese, Chromatographie, Analytik und vielen mehr..

Setzen Sie sich mit dem technischen Dienst in Verbindung.