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haemtech含氟底物

 更新時(shí)間:2020-07-03 點(diǎn)擊量:1233

Fluorogenic Substrates

haemtech含氟底物

基于ANSN的成花底物的一般結(jié)構(gòu)
闡述了6-氨基-1-萘磺酰胺(ANSN)熒光底物的一般結(jié)構(gòu)。在目前的化合物家族中,R1是一種三肽,其COOH末端殘基通常是精氨酸。R2和R3可以是氫、烷基、芳基或環(huán)烷基。虛線表示各種絲氨酸蛋白酶水解的位置。

含有熒光報(bào)告基團(tuán)6-氨基-1-萘磺酰胺(ANSN)的底物是監(jiān)測(cè)各種絲氨酸蛋白酶(1-12)酶活性的有用化合物。在這類化合物中,ANSN報(bào)告基團(tuán)(在R1位置)與短的三肽序列相連。肽序列的設(shè)計(jì)是為了優(yōu)化酶和底物之間的相互作用??梢蕴砑拥絉2和R3位置的附加組分反映了P'亞基位置的變化,并且通常會(huì)影響底物的動(dòng)力學(xué)參數(shù)。作為有效底物的化合物在三肽和ANSN基團(tuán)之間水解。一旦從肽段分離,ANSN基團(tuán)的相對(duì)熒光強(qiáng)度增加了約1000倍。
下頁確定的動(dòng)力學(xué)特性將有助于選擇合適的底物。ANSN底物被證明特別適用于因子VIIa(1-5,7,9,10,12)的分析。盡管僅因子VIIa的底物水解速率相對(duì)較慢,但當(dāng)將組織因子納入分析系統(tǒng)時(shí),化合物SN-17a等幾種化合物的kcat發(fā)生了很大變化。
使用信息:
在二甲基亞砜中,以10mM的儲(chǔ)備溶液形式提供基于ANSN的底物,通常用于分析濃度范圍為400 nM至50pM的酶。ANSN底物通常在50至100µM的終濃度下使用,并且可以在大多數(shù)生理緩沖液(即TBS、HBS、PBS等)中稀釋到該終濃度。反應(yīng)(熒光的相對(duì)變化)可使用標(biāo)準(zhǔn)熒光計(jì)或熒光板閱讀器進(jìn)行監(jiān)測(cè)。儀器設(shè)置在以下波長(zhǎng)(激發(fā)=352nm,發(fā)射=470nm)時(shí),可以使用動(dòng)力學(xué)或端點(diǎn)模式。通過在發(fā)射光束中使用390到450nm長(zhǎng)通截止濾波器,可以將光偽影小化。

下表列出了每種基質(zhì)的動(dòng)力學(xué)特性,下表列出了使用實(shí)例的期刊參考文獻(xiàn)列表。
二甲基亞砜中的儲(chǔ)備基質(zhì)溶液應(yīng)在4°C或更低溫度下冷凍保存,并應(yīng)避光。在這些條件下,化合物將保持穩(wěn)定一年以上。
**下表關(guān)鍵字:Km=µM;kcat=s-1;kcat/Km=M-1s-1 x 10-5;ND=未確定

 

  •  SN-5 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire
    StructureD-AFK-ANSNH-iC4H9.2HBr
    Useful ForUseful for plasmin
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KMNDNDNDNDNDNDND130
    KcatNDNDNDNDNDNDND3.7
    Kcat/KMNDNDNDNDNDNDND0.28
  •  SN-7 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     

    StructureMes-D-LGR-ANSN(C2H5)2
    Useful ForUseful for factor Xa
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KM31180200125580113NDND
    Kcat0.630.0070.7936150.055NDND
    Kcat/KM0.2ND0.042.90.260.005NDND
  •  SN-13a 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     

    StructureD-LPR-ANSNH-C3H7 • 2 HCl
    Useful ForUseful for factor XIa
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KM0.5300300171754598ND
    Kcat190.074.53.353520.31ND
    Kcat/KM3800.0020.150.197.1120.03ND
  •  SN-17a 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     

    StructureD-FPR-ANSNH-C6H11 • 2 HCl
    Useful ForUseful for Thrombin & VIIa
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KM0.4150330150ND7.836ND
    Kcat170.058.40.32ND6.60.074ND
    Kcat/KM4300.0040.250.02ND8.60.02ND
  •  SN-17c 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     

    StructureD-FPR-ANSNH-C4H9 • 2 HCl
    Useful ForUseful for factor VIIa
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KMND186102NDND53NDND
    KcatND0.112.7NDND21NDND
    Kcat/KMND0.0060.26NDND4NDND
  •  SN-18 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     SAFETY DATA SHEET

    StructureBoc-L-(p-F)FPR-ANSNH-C2H5
    Useful ForUseful for tPA
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KM3.750217NDNDND71ND
    Kcat440.0080.88NDNDND1.03ND
    Kcat/KM1200.0020.04NDNDND0.15ND
  •  SN-20 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     SAFETY DATA SHEET

    StructureBoc-L-FPR-ANSNH-C2H5
    Useful ForUseful for thrombin
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KM17NDND100ND54047ND
    Kcat58NDND0.31ND2.20.011ND
    Kcat/KM34NDND0.003ND0.040.002ND
  •  SN-45 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     SAFETY DATA SHEET

    StructureL-EGR-ANSNH-C3H7 • 2 HBr
    Useful ForUseful for factor XIa
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KM100NDND110225440NDND
    Kcat2.5NDND0.28217NDND
    Kcat/KM0.25NDND0.023.60.39NDND
  •  SN-54 6-ami-naphthalenesulfonamide-based (ANSN) fluorogenic substratePricing: Please Inquire

     

    StructureBOC-D-VLR-ANSNH-C4H9
    Useful ForUseful for aPC
    FormulationDMSO
    Concentration10 mM
    Kinetic PropertiesIIaVIIaVIIa/TFXaXIaaPCtPAPlasmin
    KM194217019ND3.9NDND
    Kcat0.0550.0071.60.055ND2.1NDND
    Kcat/KM0.030.0020.090.03ND5.2NDND