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    1. Metabolic Enzyme/Protease
    2. Glucokinase

    Glucokinase activator 1 

    目录号: HY-101788
    产品使用指南

    Glucokinase activator 1 是针对肝脏的葡萄糖激酶活化剂,EC50 为34 nM。

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    Glucokinase activator 1 Chemical Structure

    Glucokinase activator 1 Chemical Structure

    CAS No. : 1328987-85-4

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    Description

    Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.

    IC50 & Target

    EC50: 34 nM (Glucokinase)[1]

    In Vivo

    Glucokinase activator 1 (3 to 300 mg/kg, oral, 180 minutes) shows a dose dependent improvement in glucose excursion in oGTT in a DIO mouse model of T2D. The predominant liver-directed tissue distribution of Glucokinase activator 1 ensures a good safety window with respect to hypoglycemia over a 10-fold dose range[1].

    Animal Model: Male C57BL/6J mice (age 8-10 weeks; 25±5 g)[1]
    Dosage: 1 or 3 mg/kg (i.v.), 30 mg/kg (oral)
    Administration: i.v. or oral
    Result: Glucokinase activator 1 shows an excellent PK profile and exhibited 35- and 68- fold higher liver concentrations at 1 and 3 h time point, respectively, compared with plasma[1].
    Animal Model: Male C57BL/6J mice of 10-12 weeks[1]
    Dosage: 3 to 300 mg/kg
    Administration: Oral (15, 30, 60, 120 and 180 minutes)
    Result: Glucokinase activator 1 demonstrates 21% and 34% significant AUCglucose reduction at oral dose of 30 and 100 mg/kg, respectively[1].
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7048 mL 8.5240 mL 17.0480 mL
    5 mM 0.3410 mL 1.7048 mL 3.4096 mL
    10 mM 0.1705 mL 0.8524 mL 1.7048 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    586.58

    Formula

    C??H??F?N?O?S?

    CAS No.

    1328987-85-4

    SMILES

    O=S(C1=CC=C([C@H](C(NC2=NC=C(OC3=CC=C(C(O)=O)C=C3)S2)=O)OC4=CC=C(F)C=C4F)C=C1)(C5CC5)=O

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

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    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    Glucokinase activator 1
    目录号:
    HY-101788
    需求量:

    Glucokinase activator 1

    Cat. No.: HY-101788

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