LCZ960
LCZ960 is an orally active glucokinase (GK) activator. LCZ960 stimulates GK activity in hepatocytes in vitro and stimulates glucose uptake in vivo through hepatic GK activation. LCZ960 lowers blood glucose in mice with diet-induced obesity (DIO). LCZ960 maintains normoglycemia and improves glucose tolerance in DIO mice and rats. LCZ960 stimulates glycogen synthase flux and increases hepatic glycogen turnover in rats. LCZ960 induces increased hepatic glycogen recycling. LCZ960 can be used to study high-fat diet-induced obesity and type 2 diabetes.
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- CAS No.: 1067877-83-1
- 화학식: C30H34N6O3S2
- 분자량:590.76
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
LCZ960 (0-30 mg/kg, p.o., once a day, 7 days) decreases blood glucose levels and improves glucose excursion in DIO rat model[1].
LCZ960 (60 mg/kg, p.o., once) increases hepatic glycogen storage, glycogen synthesis (Vsyn), glycogen breakdown, hepatic glycogen turnover, hepatic glycogen, plasma glucose, suppressed plasma lactate concentrations.in SD rat model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DIO mice (male C57Bl/6, 23-32 g) model[1]
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Dosage:30 mg/kg
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Administration:p.o. once/once a day, 18 days
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Result:Increased the liver over plasma levels.
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Animal Model:DIO mice (male C57Bl/6, 23-32 g) model[1]
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Dosage:0, 10, 30, 100 and 300 mg/kg
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Administration:p.o., once/once a day, 2 weeks
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Result:Showed dose-dependent blood glucose reduction over 24 h without reaching the hypoglycemic state, even at a very high dose of 300 mg/kg, did not lower fasting blood glucose into the hypoglycemic range.
Dose-dependent improved glucose tolerance at 2 weeks, decreased insulin AUC at 100 mg/kg.
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Animal Model:DIO rat (male SD, 480 g) model[1]
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Dosage:0, 10, 30 mg/kg
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Administration:p.o., once a day, 7 days
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Result:Decreased blood glucose levels and improved glucose excursion (significant at 30 mg/kg) at day 7.
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Animal Model:SD rat (male SD, 480 g) model[1]
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Dosage:60 mg/kg
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Administration:p.o., once
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Result:Did not further increase glucose-stimulated G6P accumulation but clearly augmented hepatic glycogen storage during the first 2 h of infusion.
Increased the true rate of glycogen synthesis (Vsyn), glycogen breakdown, hepatic glycogen turnover, hepatic glycogen concentrations, plasma glucose concentrations, suppressed plasma lactate concentrations.
Chemical Information
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CAS No. 1067877-83-1
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분자량 590.76
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화학식 C30H34N6O3S2
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SMILES
O=S(C(C=C1)=CC=C1[C@@H](CC2CCCC2)C(NC3=NC4=CC=C(C5=CC=NC=C5)N=C4S3)=O)(N6CCN(CC6)C)=O
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Synonyms
NVP-LCZ960
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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