2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. Talabostat

Talabostat  (Synonyms: Val-boroPro; PT100)

目录号: HY-13233
产品使用指南

摩尔计算器

Talabostat (Val-boroPro; PT100) 是一种口服活性和非选择性的二肽基肽酶 IV (DPP-IV) 抑制剂 (IC50 < 4 nM; Ki = 0.18 nM) 和成纤维细胞活化蛋白 (FAP) 的第一个临床抑制剂 (IC50 = 560 nM)，抑制 DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM)，静息细胞脯氨酸二肽酶 (QPP) (IC50 = 310 nM)、DPP2 和一些其他 DASH 家族酶。具有抗肿瘤和造血刺激活性 。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Talabostat Chemical Structure

Talabostat Chemical Structure

CAS No. : 149682-77-9

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Talabostat 的其他形式现货产品:

Customer Review

Other Forms of Talabostat:

Talabostat 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 35 篇科研文献

WB

    Talabostat purchased from MCE. Usage Cited in: J Biol Chem. 2018 Dec 7;293(49):18864-18878.  [Abstract]

    Lack of evidence for directly binding to NLRP1 by Talabostat. 293T-ASC-GFPNLRP1 cells are treated with 2 μM Talabostat for 16 hours and lysed by 3 rounds of freezing and thawing. 20 μL (2 μg/uL) clarified lysates are heated at a temperature gradient for 10 minutes, centrifuged at 16,000g for 10mins at room temperature.

    查看 Dipeptidyl Peptidase 亚型特异性产品:

    查看所有亚型
    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

    Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities[1][2][3].

    IC50 & Target

    IC50: < 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP)[1]
    Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9)[2]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 IC50
    0.066 μM
    Compound: 1, PT-100
    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
    0.066 μM
    Compound: 1, PT-100, Val-boroPro
    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]
    HEK293 IC50
    0.07 μM
    Compound: 1, PT- 100, Talabostat
    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]
    HEK-293T IC50
    6.8 μM
    Compound: 1, Val-boroPro
    Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs
    Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs
    		[PMID: 18783201]
    U-87MG ATCC IC50
    0.224 μM
    Compound: Talabostat
    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]
    体外研究
    (In Vitro)

    By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat (Val-boroPro) inhibits dipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity[3].
    Talabostat (Val-boroPro) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site[4].

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

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

    Talabostat (Val-boroPro; PT100) can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system.
    In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, Talabostat (Val-boroPro) causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory.
    Talabostat (Val-boroPro) treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[4].

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

    214.07

    Formula

    C9H19BN2O3
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 40 mg/mL (186.85 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 4.6714 mL 23.3568 mL 46.7137 mL
    5 mM 0.9343 mL 4.6714 mL 9.3427 mL
    查看完整储备液配制表

    • 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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献
    Animal Administration
    [4]

    Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostrils of male mice. Talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed before BLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvested for histological and quantitative real-time polymerase chain reaction (qRT-PCR) analyses[4].

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

    Talabostat 相关分类

    完整储备液配制表

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.6714 mL 23.3568 mL 46.7137 mL 116.7842 mL
    5 mM 0.9343 mL 4.6714 mL 9.3427 mL 23.3568 mL
    10 mM 0.4671 mL 2.3357 mL 4.6714 mL 11.6784 mL
    15 mM 0.3114 mL 1.5571 mL 3.1142 mL 7.7856 mL
    20 mM 0.2336 mL 1.1678 mL 2.3357 mL 5.8392 mL
    25 mM 0.1869 mL 0.9343 mL 1.8685 mL 4.6714 mL
    30 mM 0.1557 mL 0.7786 mL 1.5571 mL 3.8928 mL
    40 mM 0.1168 mL 0.5839 mL 1.1678 mL 2.9196 mL
    50 mM 0.0934 mL 0.4671 mL 0.9343 mL 2.3357 mL
    60 mM 0.0779 mL 0.3893 mL 0.7786 mL 1.9464 mL
    80 mM 0.0584 mL 0.2920 mL 0.5839 mL 1.4598 mL
    100 mM 0.0467 mL 0.2336 mL 0.4671 mL 1.1678 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:

    Talabostat149682-77-9Val-boroPro PT100PT100PT 100PT-100Dipeptidyl PeptidaseDPPInhibitorinhibitorinhibit

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * 需求量：

    * 客户姓名：

    		 

    * Email：

    * 电话：

    		 

    * 公司或机构名称：

       留言给我们：

    Bulk Inquiry

    Inquiry Information

    产品名称：
    Talabostat
    目录号：
    HY-13233
    需求量：

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * Lot #：

    * 客户姓名：

    		 

    * Email：

       电话：

    		 

    * 部门：

    * 公司或机构名称：

    		 

       留言给我们：

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.

    嗨！很高兴为您提供帮助！

    尊敬的 MCE 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z