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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1067877-83-1
- 分子式: C30H34N6O3S2
- 分子量:590.76
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 1067877-83-1
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分子量 590.76
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分子式 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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別名
NVP-LCZ960
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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