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5.04377

Sigma-Aldrich

AMPK Signaling Activator XIII, ZLN005

Synonym(e):

AMPK Signaling Activator XIII, ZLN005, 2-(4- tert-Butylphenyl)-1H-benzo[d]imidazole, 2-(4-(2-Methyl-2-propanyl)phenyl)-1H-benzimidazole, Luciferase Inhibitor IV, 2-(4-tert-Butylphenyl)-1H-benzo[d]imidazole, 2-(4-(2-Methyl-2-propanyl)phenyl)-1H-benzimidazole, Luciferase Inhibitor IV

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About This Item

Empirische Formel (Hill-System):
C17H18N2
CAS-Nummer:
Molekulargewicht:
250.34
UNSPSC-Code:
12352200
NACRES:
NA.77

Assay

≥99% (HPLC)

Qualitätsniveau

Form

powder

Hersteller/Markenname

Calbiochem®

Lagerbedingungen

OK to freeze
protect from light

Farbe

pink-white

Löslichkeit

DMSO: 50 mg/mL

Lagertemp.

2-8°C

InChI

1S/C17H18N2/c1-17(2,3)13-10-8-12(9-11-13)16-18-14-6-4-5-7-15(14)19-16/h4-11H,1-3H3,(H,18,19)

InChIKey

LQUNNCQSFFKSSK-UHFFFAOYSA-N

Allgemeine Beschreibung

A cell-permeable benzimidazole that, in addition to its inhibitory potency against luciferase activity (IC50<10 nM), also activates AMPK signaling by increasing cellular ADP/ATP ratio via mitochondria respiration upcoupling, effectively activating AMPK & PGC-1α in muscle, but not liver, cell types both in cultures (5-20 µM in rat L6 myotubes) in vitro and in db/db mice (15 mg/kg/day via p.o.) in vivo. Reported to improve glucose and insulin tolerance of db/db mice without any apparent effects on body weight or food intake.
A cell-permeable benzimidazole that, in addition to its inhibitory potency against luciferase activity (IC50<10 nM), is reported to activate AMPK signaling by increasing cellular ADP/ATP ratio via mitochondria respiration uncoupling in a cell type-specific manner, effectively activating AMPK & PGC-1α in muscle, but not liver, cell types both in cultures (5-20 µM & 1-24 h in rat L6 myotubes; no effect in primary rat hepatocytes) in vitro and in db/db mice (gastrocnemius/calf muscle, but not liver tissue; 15 mg/kg/day via p.o. for 6 wks) in vivo. ZLN005 is orally available in mice (plasma Cmax & Tmax = 3.7 µM & 15 min, respectively, following single 15 mg/kg oral dosage to db/db mice) and is efficacious in improving glucose (1.5 g/kg i.p.) tolerance among 4-wk-treated and insulin (1 unit/kg) tolerance among 5-wk treated db/db mice (by 14% and 18%, respectively; 15 mg/kg/day via p.o.) in vivo without any apparent effects on body weight or food intake among db/db or non-diabetic controls.

Biochem./physiol. Wirkung

Cell permeable: yes
Primary Target
increases cellular ADP/ATP ratio via mitochondria respiration uncoupling
Secondary Target
luciferase activity inhibitor

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Sonstige Hinweise

Zhang, L.N., et al. 2013. Diabetes.62, 1297.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3


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