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

Vildagliptin  (Synonyms: 維格列汀; LAF237; NVP-LAF 237)

目錄號(hào): HY-14291 純度: 99.61%
COA 產(chǎn)品使用指南

Vildagliptin (LAF237) 是一種有效且穩(wěn)定的選擇性二肽基肽酶IV (DPP-IV) 抑制劑，在人 Caco-2 細(xì)胞中抑制 DPP-IV 的 IC50 為 3.5 nM。Vildagliptin 具有出色的口服生物利用度和有效的降血糖活性。

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Vildagliptin Chemical Structure

Vildagliptin Chemical Structure

CAS No. : 274901-16-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in Water ￥660
In-stock
5 mg ￥371
In-stock
10 mg ￥600
In-stock
50 mg ￥1200
In-stock
100 mg ￥1700
In-stock
500 mg ￥3500
In-stock
1 g   詢(xún)價(jià)  
5 g   詢(xún)價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Vildagliptin:

    Vildagliptin purchased from MCE. Usage Cited in: Int J Mol Sci. 2022, 23(22), 14101

    qPCR Assay. Vildagliptin (5 μM; 0, 6, 12, 24, 48, 72 h) stimulates the expression of IL-6 in HaCaT cells.

    Vildagliptin purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:26-37.  [Abstract]

    Representative images showing visible metastatic nodules in the lungs of mice treated with Vildagliptin and fed an high-fat diet (HFD).

    查看 Dipeptidyl Peptidase 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].

    IC50 & Target

    DPP-4

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Caco-2 IC50
    62 nM
    Compound: Vildagliptin
    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]
    HEK293 IC50
    52 μM
    Compound: 3
    Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
    Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
    		[PMID: 22525314]
    Sf9 IC50
    0.14 μM
    Compound: Vildagliptin
    Inhibition of recombinant full-length human N-terminal GST-tagged DPP9 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay
    Inhibition of recombinant full-length human N-terminal GST-tagged DPP9 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay
    		[PMID: 30642693]
    Sf9 IC50
    2.3 μM
    Compound: Vildagliptin
    Inhibition of recombinant full-length human N-terminal GST-tagged DPP8 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay
    Inhibition of recombinant full-length human N-terminal GST-tagged DPP8 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay
    		[PMID: 30642693]
    U-87MG ATCC IC50
    79.76 μM
    Compound: Vildagliptin
    Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
    Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
    		[PMID: 32527554]
    體外研究
    (In Vitro)

    Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation[2].

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

    Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice[2].
    Vildagliptin (10 μmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats[1].

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

    Animal Model: Male db/db mice (BKS) and wildtype mice[2]
    Dosage: 35 mg/kg
    Administration: Oral gavage; once daily; for 6 weeks
    Result: Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44).
    Animal Model: Obese male Zucker rats[1]
    Dosage: 10 μmol/kg (Pharmacokinetic Analysis)
    Administration: Orally
    Result: Significantly decreased glucose excursions and stimulate insulin secretion.
    Clinical Trial
    分子量

    303.40

    Formula

    C17H25N3O2
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱(chēng)

    維達(dá)列??；維格列汀
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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)： 

    H2O 中的溶解度 : 50 mg/mL (164.80 mM; 超聲助溶)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.2960 mL 16.4799 mL 32.9598 mL
    5 mM 0.6592 mL 3.2960 mL 6.5920 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 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)：

    以下溶解方案，請(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： PBS

      Solubility: 100 mg/mL (329.60 mM); 澄清溶液; 超聲助溶 (<60°C)

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)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(guò)程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?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
    H2O 1 mM 3.2960 mL 16.4799 mL 32.9598 mL 82.3995 mL
    5 mM 0.6592 mL 3.2960 mL 6.5920 mL 16.4799 mL
    10 mM 0.3296 mL 1.6480 mL 3.2960 mL 8.2399 mL
    15 mM 0.2197 mL 1.0987 mL 2.1973 mL 5.4933 mL
    20 mM 0.1648 mL 0.8240 mL 1.6480 mL 4.1200 mL
    25 mM 0.1318 mL 0.6592 mL 1.3184 mL 3.2960 mL
    30 mM 0.1099 mL 0.5493 mL 1.0987 mL 2.7466 mL
    40 mM 0.0824 mL 0.4120 mL 0.8240 mL 2.0600 mL
    50 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6480 mL
    60 mM 0.0549 mL 0.2747 mL 0.5493 mL 1.3733 mL
    80 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0300 mL
    100 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8240 mL

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    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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    產(chǎn)品名稱(chēng)：
    Vildagliptin
    目錄號(hào)：
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