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

Linagliptin  (Synonyms: 利格列汀; BI 1356)

目錄號: HY-10284 純度: 99.91%
COA 產(chǎn)品使用指南 技術(shù)支持

Linagliptin 是一種有效，選擇性的 DPP-4 抑制劑，IC50 值為 1 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Linagliptin Chemical Structure

Linagliptin Chemical Structure

CAS No. : 668270-12-0

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
In-stock
100 mg ￥480
In-stock
500 mg ￥760
In-stock
1 g ￥1290
In-stock
5 g   詢價(jià)  
10 g   詢價(jià)  

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Customer Review

Other Forms of Linagliptin:

    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 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

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

    IC50 & Target

    DPP-4

     

    細(xì)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]
    體外研究
    (In Vitro)

    Linagliptin inhibits DPP-4 activity in vitro in several independent experiments with IC50 values of 0.4, 0.5, 0.9, and 1.1 nM (mean IC50, approximately 1 nM). Linagliptin inhibits FAP with an IC50 of 89 nM (approximately 90-fold selectivity versus DPP-4)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    In male Wistar rats, Beagle dogs, and Rhesus monkeys, xanthine linagliptin proves to be a highly efficacious, long-lasting, and potent DPP-4 inhibitor providing >70% inhibition for >7 h for all three species after oral administration of 1 mg/kg. Single oral administration of linagliptin to db/db mice 45 min prior to an oral glucose tolerance test reduced plasma glucose excursion in a dose-dependent manner from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition)[1]. Linagliptin (3 and 10 mg/kg) dose-dependently inhibits the DPP-4 enzyme in plasma within 30 min of administration. Linagliptin (1 mg/kg, p.o.) significantly reduces glucose excursion by approximately 50%[2]. Oral administration of the DPP-4 inhibitor linagliptin (3 mg/kg, p.o.) strongly reduces DPP-4 activity, stabilizes active GLP-1 in chronic wounds, and improves healing in ob/ob mice. At day 10 postwounding, linagliptin-treated ob/ob mice show largely epithelialized wounds characterized by the absence of neutrophils[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 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    利格列?。焕。焕窭?/p>
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 25 mg/mL (52.91 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 25 mg/mL (52.91 mM); 澄清溶液

      此方案可獲得 ≥ 25 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      以 1 mL 工作液為例，取 100 μL 250.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

    • 方案 二

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (5.29 mM); 澄清溶液; 超聲助溶

      此方案可獲得 2.5 mg/mL的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 5 mg/mL (10.58 mM); 澄清溶液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.91%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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    產(chǎn)品名稱：
    Linagliptin
    目錄號：
    HY-10284
    需求量：