1. Membrane Transporter/Ion Channel
  2. SGLT
  3. Dapagliflozin

Dapagliflozin  (Synonyms: 达格列净; BMS-512148)

目录号: HY-10450 纯度: 99.89%
COA 产品使用指南

Dapagliflozin (BMS-512148) 是一种竞争性葡萄糖协同转运蛋白2 (SGLT2) 抑制剂,可导致尿液中葡萄糖的排泄,用于糖尿病 (DM) 的研究。Dapagliflozin 诱导 HIF1 表达并减轻肾脏 IR 损伤。

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Dapagliflozin Chemical Structure

Dapagliflozin Chemical Structure

CAS No. : 461432-26-8

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥825
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5 mg ¥750
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10 mg ¥1100
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50 mg ¥2750
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100 mg ¥4500
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 31 篇科研文献

WB
Cell Viability Assay
IF

    Dapagliflozin purchased from MCE. Usage Cited in: Life Sci. 2023 Apr 4;121671.  [Abstract]

    Dapagliflozin (DAPA; 10 μM; 24 hours) significantly reduces the high glucose-induced increase in YAP/TAZ expression in HK-2 cells.

    Dapagliflozin purchased from MCE. Usage Cited in: Life Sci. 2023 Apr 4;121671.  [Abstract]

    Dapagliflozin (DAPA; 10, 20 μM; 24 h) significantly reverses the decrease in cell viability caused by high glucose in HK-2 cells.

    Dapagliflozin purchased from MCE. Usage Cited in: Life Sci. 2023 Apr 4;121671.  [Abstract]

    Dapagliflozin (DAPA; 10 μM; 24 hours) significantly decreases the expression of YAP/TAZ and increases the ratios of p-YAP/YAP and pTAZ/TAZ under high glucose conditions in HK-2 cells.

    Dapagliflozin purchased from MCE. Usage Cited in: EBioMedicine. 2022, 86: 104342.

    Dapagliflozin increases the LC3-II to LC3-I expression ratio in the liver.

    Dapagliflozin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Jun;152:45-59.  [Abstract]

    Effects of Dapagliflozin and Empagliflozin on p62 expression in LPS-untreated and LPS-treated RAW264.7 cells.

    Dapagliflozin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;45(5):1747-1758.  [Abstract]

    The expression of IRS1 significantly decreases. The phosphorylation levels of Akt1, Akt2, and S6 are significantly reduced in livers of db/db mice.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine[1]. Dapagliflozin induces HIF1 expression and attenuates renal IR injury[2].

    IC50 & Target

    SGLT2

     

    体外研究
    (In Vitro)

    Dapagliflozin (0-10 μM;24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner[2].
    Dapagliflozin (0-10 μM;2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells[2]..

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[1]

    Cell Line: Hypoxic HK2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 5 μM, 10 μM
    Incubation Time: 24 hours
    Result: Improved the cell viability in a dose-dependent manner compared with control cells.

    Western Blot Analysis[1]

    Cell Line: Hypoxic HK2 cells, Normoxic HK2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 5 μM, 10 μM
    Incubation Time: 24 hours
    Result: Induced HIF1 expression in hypoxic and normoxic HK2 cells.
    体内研究
    (In Vivo)

    Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    408.87

    Formula

    C21H25ClO6

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    达格列净;达帕格列净;达格列嗪

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (244.58 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 50 mg/mL (122.29 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4458 mL 12.2288 mL 24.4577 mL
    5 mM 0.4892 mL 2.4458 mL 4.8915 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (6.11 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.11 mM); 澄清溶液

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 33.33 mg/mL (81.52 mM); 澄清溶液; 超声助溶 (<60°C)

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.89%

    参考文献

    Dapagliflozin 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.4458 mL 12.2288 mL 24.4577 mL 61.1441 mL
    5 mM 0.4892 mL 2.4458 mL 4.8915 mL 12.2288 mL
    10 mM 0.2446 mL 1.2229 mL 2.4458 mL 6.1144 mL
    15 mM 0.1631 mL 0.8153 mL 1.6305 mL 4.0763 mL
    20 mM 0.1223 mL 0.6114 mL 1.2229 mL 3.0572 mL
    25 mM 0.0978 mL 0.4892 mL 0.9783 mL 2.4458 mL
    30 mM 0.0815 mL 0.4076 mL 0.8153 mL 2.0381 mL
    40 mM 0.0611 mL 0.3057 mL 0.6114 mL 1.5286 mL
    50 mM 0.0489 mL 0.2446 mL 0.4892 mL 1.2229 mL
    60 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0191 mL
    80 mM 0.0306 mL 0.1529 mL 0.3057 mL 0.7643 mL
    100 mM 0.0245 mL 0.1223 mL 0.2446 mL 0.6114 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

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