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

LCZ960 是一种具有口服活性的葡萄糖激酶 (Glucokinase) (GK) 激活剂。LCZ960 在体外对肝细胞中的 GK 活性发挥刺激作用，在体内通过肝脏 GK 激活刺激葡萄糖摄取。LCZ960 可降低饮食诱导肥胖 (DIO) 小鼠的血糖剂量。LCZ960 维持 DIO 小鼠和大鼠的正常血糖并改善了葡萄糖耐量。LCZ960 在大鼠中刺激糖原合酶通量，肝糖原周转增加。LCZ960 诱导肝糖原循环增加。LCZ960 可用于研究高脂饮食导致的肥胖和 2 型糖尿病。

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LCZ960

LCZ960 Chemical Structure

CAS No. : 1067877-83-1

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LCZ960 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体内研究
(In Vivo)

LCZ960 (0-300 mg/kg，口服，单次/每日一次，14-18 天) 在饮食诱导性肥胖 (DIO) 小鼠模型中可提高肝糖原过量血浆水平和葡萄糖耐量，降低血糖[1]。
LCZ960 (0-30 mg/kg，口服，每日一次，7 天) 可降低 DIO 大鼠模型中的血糖水平并改善血糖波动[1]。
LCZ960 (60 mg/kg，口服，一次) 可增加 SD 大鼠模型中的肝糖原储存、糖原合成 (Vsyn)、糖原分解、肝糖原周转、肝糖原、血浆葡萄糖，并抑制血浆乳酸浓度[1]。

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.
分子量

590.76

Formula

C30H34N6O3S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

LCZ960 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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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