5.04377

AMPK Signaling Activator XIII, ZLN005

• 동의어(들): 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
• 실험식(Hill 표기법): C₁₇H₁₈N₂
• CAS Number: 4529-96-8
• Molecular Weight: 250.34
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥99% (HPLC)
• Quality Level: 100
• 형태: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: pink-white
• solubility: DMSO: 50 mg/mL
• 저장 온도: 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)
• InChI key: LQUNNCQSFFKSSK-UHFFFAOYSA-N

설명

일반 설명

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 C_max & T_max = 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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
increases cellular ADP/ATP ratio via mitochondria respiration uncoupling

Secondary Target
luciferase activity inhibitor

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3