2. Metabolic Enzyme/Protease Autophagy Apoptosis
  3. Dipeptidyl Peptidase Autophagy Ferroptosis
  4. Linagliptin

Linagliptin  (Synonyms: 利格列汀; BI 1356)

目录号: HY-10284 纯度: 99.91%
COA 产品使用指南 技术支持

Linagliptin 是一种有效，选择性的 DPP-4 抑制剂，IC50 值为 1 nM。

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Linagliptin

Linagliptin Chemical Structure

CAS No. : 668270-12-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
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100 mg ￥480
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500 mg ￥760
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1 g ￥1290
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Customer Review

Other Forms of Linagliptin:

Linagliptin 相关抗体

Top Publications Citing Use of Products

    Linagliptin purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 28;7(1):4351.  [Abstract]

    Western blot analysis of CREB protein phosphorylation in pancreas of KKAy mice treated with HBK001 and Linagliptin.

    查看 Dipeptidyl Peptidase 亚型特异性产品:

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    DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

    IC50 & Target

    DPP-4

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Caco-2 IC50
    1 nM
    Compound: XV, Trajenta
    Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay
    Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay
    		[PMID: 23623674]
    Caco-2 IC50
    1 nM
    Compound: B1 1356
    Inhibition of DPP4 in human Caco-2 cells after 1 hr
    Inhibition of DPP4 in human Caco-2 cells after 1 hr
    		[PMID: 18485703]
    Caco-2 IC50
    1 nM
    Compound: 1, BI 1356
    Inhibition of human DPP4 in Caco-2 cells by fluorescene assay
    Inhibition of human DPP4 in Caco-2 cells by fluorescene assay
    		[PMID: 18052023]
    HEK293 IC50
    > 100 μM
    Compound: Linagliptin
    Inhibition of OAT3 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E-sul substrate uptake by liquid scintillation counting
    Inhibition of OAT3 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E-sul substrate uptake by liquid scintillation counting
    		[PMID: 23073734]
    HEK293 IC50
    > 100 μM
    Compound: Linagliptin
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E217betaG substrate uptake by liquid scintillation counting
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E217betaG substrate uptake by liquid scintillation counting
    		[PMID: 23073734]
    HEK293 IC50
    0.37 μM
    Compound: 2
    Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
    Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
    		[PMID: 24617858]
    HEK293 IC50
    0.37 μM
    Compound: 2,BI 1356, linagliptin, Tradjenta
    Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
    Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
    		[PMID: 24900696]
    HEK293 IC50
    41 μM
    Compound: Linagliptin
    Inhibition of OCT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting
    Inhibition of OCT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting
    		[PMID: 23073734]
    HEK293 IC50
    45 μM
    Compound: Linagliptin
    Inhibition of OCT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [ethyl 1-14C]TEA substrate uptake at 100 uM by liquid scintillation counting
    Inhibition of OCT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [ethyl 1-14C]TEA substrate uptake at 100 uM by liquid scintillation counting
    		[PMID: 23073734]
    HEK293 IC50
    80 μM
    Compound: Linagliptin
    Inhibition of OCT2 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting
    Inhibition of OCT2 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting
    		[PMID: 23073734]
    LLC-PK1 IC50
    66.1 μM
    Compound: Linagliptin
    Inhibition of human P-glycoprotein expressed in pig LLC-PK1 cells assessed as reduction of [3H]digoxin substrate transport from basolateral to apical side by liquid scintillation counting
    Inhibition of human P-glycoprotein expressed in pig LLC-PK1 cells assessed as reduction of [3H]digoxin substrate transport from basolateral to apical side by liquid scintillation counting
    		[PMID: 23073734]
    体外研究
    (In Vitro)

    Linagliptin 在多项独立体外实验中可抑制 DPP-4 活性，其 IC50 分别为 0.4、0.5、0.9 和 1.1 nM，平均 IC50 约为 1 nM。Linagliptin 抑制 FAP 的 IC50 为 89 nM，相较于 DPP-4 具有约 90 倍的选择性[2]。

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

    Linagliptin 相关抗体:
    体内研究
    (In Vivo)

    在雄性 Wistar 大鼠、Beagle 犬和恒河猴中，黄嘌呤类化合物 Linagliptin 表现出高效、持久且强效的 DPP-4 抑制作用，在口服 1 mg/kg 后三种动物均可维持超过 70% 的 DPP-4 抑制率达 7 小时以上[1]。在口服葡萄糖耐量试验前 45 分钟单次口服给予 Linagliptin 可剂量依赖性地降低 db/db 小鼠的血糖波动，其抑制率从 0.1 mg/kg (15%) 增加至 1 mg/kg (66%)[1]。Linagliptin (3 和 10 mg/kg) 在给药 30 分钟内可剂量依赖性地抑制血浆中 DPP-4 酶活性。Linagliptin (1 mg/kg，灌胃) 可显著降低约 50% 的血糖波动[2]。DPP-4 抑制剂 Linagliptin (3 mg/kg，灌胃) 的口服给药可显著降低 DPP-4 活性，稳定慢性创口中活性 GLP-1 的水平，并促进 ob/ob 小鼠创伤愈合。在伤后第 10 天，Linagliptin 处理组的 ob/ob 小鼠创面基本实现上皮化，且几乎无中性粒细胞浸润[3]。

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

    472.54

    Formula

    C25H28N8O2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    利格列汀；利拉利汀；利格利汀
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 25 mg/mL (52.91 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1162 mL 10.5811 mL 21.1622 mL
    5 mM 0.4232 mL 2.1162 mL 4.2324 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    动物实验：

    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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.29 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.29 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配制工作液。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： 50% PEG300    50% Saline

      Solubility: 5 mg/mL (10.58 mM); 澄清溶液; 超声助溶

    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

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.91%

    COA (286 KB) HNMR (270 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [3]

    EDTA plasma (20 μL) is diluted with 30 μL of DPP-4 assay buffer (100 mM Tris and 100 mM NaCl, adjusted to pH 7.8 with HCl) and mixed with 50 μL of H-Ala-Pro-7-amido-4-trifluoromethylcoumarin. The 200 mM stock solution in dimethylformamide is diluted 1:1000 with water to yield a final concentration of 100 μM. The plate is incubated at room temperature for 10 min, and fluorescence in the wells is determined by using a Victor 1420 Multilabel Counter at an excitation wavelength of 405 nm and an emission wavelength of 535 nm. For the detection of DPP-4 activity in wound lysates, 100 μg of protein from the respective wound lysates are used instead of 20 μL of plasma. Active GLP-1 is also detected from 100 μg of respective wound tissue samples and analyzed by using the Mouse/Rat Total Active GLP-1 Assay Kit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [3]

    A total of 4.0×107 keratinocytes per well are seeded into 24-well plates. After reaching 50% confluence, cells are starved for 24 h with DMEM. Proliferation of cells is assessed by using 1 μCi/mL of [3H]methyl-thymidine in DMEM in the presence of 10% fetal bovine serum and increasing concentrations of linagliptin (3, 30, 300, or 600 nM) for 24 h. Cells are then washed twice with phosphate-buffered saline and incubated in 5% trichloroacetic acid at 4°C for 30 min, and the DNA is solubilized in 0.5mol/LNaOH for 30 min at 37°C. Finally, [3H]thymidine incorporation is determined.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Each experimental group (vehicle or linagliptin treatment) consists of 10 individual ob/ob mice (n=10). Animals are treated orally once a day (8:00 AM) by gastrogavage using vehicle (1% methylcellulose) or linagliptin (3 mg/kg body weight in 1% methylcellulose) beginning 2 days (day−2) before wounding. After wounding, animals are subsequently treated once a day throughout the 10-day healing period.

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

    Linagliptin 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1162 mL 10.5811 mL 21.1622 mL 52.9056 mL
    5 mM 0.4232 mL 2.1162 mL 4.2324 mL 10.5811 mL
    10 mM 0.2116 mL 1.0581 mL 2.1162 mL 5.2906 mL
    15 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5270 mL
    20 mM 0.1058 mL 0.5291 mL 1.0581 mL 2.6453 mL
    25 mM 0.0846 mL 0.4232 mL 0.8465 mL 2.1162 mL
    30 mM 0.0705 mL 0.3527 mL 0.7054 mL 1.7635 mL
    40 mM 0.0529 mL 0.2645 mL 0.5291 mL 1.3226 mL
    50 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0581 mL
    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:

    Linagliptin668270-12-0BI 1356利格列汀利拉利汀利格利汀BI1356BI-1356Dipeptidyl PeptidaseAutophagyFerroptosisDPPInhibitorinhibitorinhibit

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