2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Prolyl Endopeptidase (PREP) FAP
  4. UAMC-1110

UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM.

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CAS 番号 : 1448440-52-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
5 mg $120 在庫あり
10 mg $192 在庫あり
25 mg $355 在庫あり
50 mg $563 在庫あり
100 mg $900 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 2 publication(s) in Google Scholar

Other Forms of UAMC-1110:

UAMC-1110 関連抗体

Top Publications Citing Use of Products

    UAMC-1110 purchased from MedChemExpress. Usage Cited in: Anal Chem. 2019 Dec 3;91(23):14873-14878.  [Abstract]

    Bioluminescence image of 50 ng/mL FAP incubated with different concentrations of SP-13786 for 60 min, then probe 1 (20 μM) is added to the mixture.

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM[1].

    IC50 & Target

    IC50: 3.2 nM (FAP), 1.8 μM (PREP)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    0.0032 μM
    Compound: 60
    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]
    U-87MG ATCC IC50
    0.055 μM
    Compound: UAMC-1110
    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]
    U-87MG ATCC IC50
    41.62 nM
    Compound: UAMC-1110
    Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate measured upto 60 mins by fluorescence based assay
    Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate measured upto 60 mins by fluorescence based assay
    		[PMID: 32527554]
    体外実験

    UAMC-1110 is also found to have better FAP/PREP selectivity and a very proficient ligand efficiency of 0.34[1].

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

    UAMC-1110 関連抗体
    体内実験

    UAMC-1110 is the most extensive and prolonged inhibitior of FAP in the PK studies. Pharmacokinetic evaluation in mice of UAMC-1110 demonstrates high oral bioavailability, plasma half-life, and the potential to selectively and completely inhibit FAP in vivo[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    344.32

    分子式

    C17H14F2N4O2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=NC2=CC=CC=C12)NCC(N3[C@H](C#N)CC(F)(F)C3)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (290.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9043 mL 14.5214 mL 29.0428 mL
    5 mM 0.5809 mL 2.9043 mL 5.8085 mL
    10 mM 0.2904 mL 1.4521 mL 2.9043 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション
    参考文献
    動物実験
    [1]

    Rats: The PK parameters are determined for inhibitors 4, 5, 60 (SP-13786), and 61 in rats. Six male rats are treated for each inhibitor tested, three of which received the compound via a single intravenous (iv) administration at 5 mg/kg. The other three animals are dosed per os (po) at 20 mg/kg. Blood samples are collected at 0.083, 0.25, 0.5, 1, 2, 4, 6, and 24 h after administration. Inhibitor concentrations are determined using UPLC−MS/MS, and pharmacokinetic parameters are calculated using standard algorithms[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.9043 mL 14.5214 mL 29.0428 mL 72.6069 mL
    5 mM 0.5809 mL 2.9043 mL 5.8086 mL 14.5214 mL
    10 mM 0.2904 mL 1.4521 mL 2.9043 mL 7.2607 mL
    15 mM 0.1936 mL 0.9681 mL 1.9362 mL 4.8405 mL
    20 mM 0.1452 mL 0.7261 mL 1.4521 mL 3.6303 mL
    25 mM 0.1162 mL 0.5809 mL 1.1617 mL 2.9043 mL
    30 mM 0.0968 mL 0.4840 mL 0.9681 mL 2.4202 mL
    40 mM 0.0726 mL 0.3630 mL 0.7261 mL 1.8152 mL
    50 mM 0.0581 mL 0.2904 mL 0.5809 mL 1.4521 mL
    60 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2101 mL
    80 mM 0.0363 mL 0.1815 mL 0.3630 mL 0.9076 mL
    100 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7261 mL
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    UAMC-1110 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    UAMC-11101448440-52-5UAMC1110UAMC 1110Prolyl Endopeptidase (PREP)FAPprolyl oligopeptidasePOPFibroblast activation proteinInhibitorinhibitorinhibit

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    製品名:
    UAMC-1110
    製品番号:
    HY-100684
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