2. Metabolic Enzyme/Protease
  3. Glucokinase
  4. 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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LCZ960

LCZ960 Chemical Structure

CAS No. : 1067877-83-1

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Description

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[1].

In Vivo

LCZ960 (0-300 mg/kg, p.o. once/once a day, 14-18 days) increases the liver over plasma levels, glucose tolerance, reduces blood glucose in diet-induced obesity (DIO) mice model[1].
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.

Animal Model: DIO mice (male C57Bl/6, 23-32 g) model[1]
Dosage: 30 mg/kg
Administration: p.o. once/once a day, 18 days
Result: Increased the liver over plasma levels.
Animal Model: DIO mice (male C57Bl/6, 23-32 g) model[1]
Dosage: 0, 10, 30, 100 and 300 mg/kg
Administration: p.o., once/once a day, 2 weeks
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.
Animal Model: DIO rat (male SD, 480 g) model[1]
Dosage: 0, 10, 30 mg/kg
Administration: p.o., once a day, 7 days
Result: Decreased blood glucose levels and improved glucose excursion (significant at 30 mg/kg) at day 7.
Animal Model: SD rat (male SD, 480 g) model[1]
Dosage: 60 mg/kg
Administration: p.o., once
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.
Molecular Weight

590.76

Formula

C30H34N6O3S2
CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LCZ960 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LCZ9601067877-83-1NVP-LCZ960LCZ 960LCZ-960GlucokinaseHexokinase IVHexokinase DActivatorDIO miceDIO ratSD ratC57Bl/6 miceInhibitorinhibitorinhibit

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