Talabostat mesylate | PT100 mesylate | Dipeptidyl Peptidase Inhibitor

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Talabostat mesylate {[allProObj[0].p_purity_real_show]}

货号：A264157 同义名： PT100 mesylate;Val-boroPro mesylate

Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) 是一种口服活性、非选择性二肽基肽酶IV（DPP-IV）抑制剂（IC50 < 4 nM；Ki = 0.18 nM），也是首个临床上抑制成纤维细胞激活蛋白（FAP）的抑制剂（IC50 = 560 nM）。它还抑制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和其他DASH家族酶，表现出抗肿瘤和造血刺激活性。

Talabostat mesylate 化学结构
CAS号：150080-09-4

Talabostat mesylate 3D分子结构
CAS号：150080-09-4

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Talabostat mesylate 纯度/质量文件产品仅供科研

货号：A264157 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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Talabostat mesylate 生物活性

描述

Dipeptidyl peptidase (DPP)-IV is a member of a family of serine peptidases that includes quiescent cell proline dipeptidase (QPP), DPP8, and DPP9; DPP-IV is a key regulator of incretin hormones. Talabostat is an inhibitor of DPP with IC_{50_{values of <4 nM, 4 nM, 11 nM, 310 nM, and 560 nM for DPP-IV, DPP8, DPP9, QPP, and FAP (fibroblast activation protein), respectively^[3]. The effects of talabostat (2 μM, 24 h) on IL-1β expression and secretion in THP-1 macrophages were determined by immunoblotting and ELISA. Talabostat modestly increased the levels of intracellular pro-IL-1β (~2-fold at 10 μM), but dramatically increased the amount of pro-IL-1β secreted into the supernatant. Talabostat induced a lytic cell death consistent with pyroptosis and inconsistent with apoptotic cell death in RAW 264.7 cells. Moreover, talabostat-treated THP-1 and RAW 264.7 cells secreted exclusively pro-caspase-1 indicating that pro-caspase-1 mediated talabostat-induced pyroptosis^[4]. In C57BL/6 female mice, 20 μg talabostat administration resulted in complete eradication of the murine bladder carcinoma following initial progression during the first week of treatment^[5].}}

Talabostat mesylate 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00489710	Kidney Cancer	Phase 2	Withdrawn(Terminated for safet... 展开 >>y reasons) 收起 <<	-	-
NCT02083120	Pulmonary Disease, Chronic Obs... 展开 >>tructive 收起 <<	Not Applicable	Active, not recruiting	November 2018	Germany ... 展开 >> Helios Klinik Ambrock Hagen, NRW, Germany, 58091 收起 <<
NCT00083239	Melanoma Skin... 展开 >> Cancer 收起 <<	Phase 2	Completed	-	United States, Georgia ... 展开 >> Emory University/Winship Cancer Institute Atlanta, Georgia, United States, 30322-1013 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109-0473 United States, New Hampshire Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756-0001 United States, Pennsylvania University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213-2582 United States, Texas Mary Crowley Medical Research Center Dallas, Texas, United States, 75246 收起 <<

Talabostat mesylate 参考文献

[1]Huang Y, Simms AE, et al. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions. Clin Exp Metastasis. 2011 Aug;28(6):567-79.

[2]Cristillo AD, Galmin L, et al. HIV-1 Env vaccine comprised of electroporated DNA and protein co-administered with Talabostat. Biochem Biophys Res Commun. 2008 May 23;370(1):22-6.

[3]Lankas GR, Leiting B, Roy RS, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005;54(10):2988-2994.

[4]Okondo MC, Johnson DC, Sridharan R, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017;13(1):46-53.

[5]Walsh MP, Duncan B, Larabee S, et al. Val-boroPro accelerates T cell priming via modulation of dendritic cell trafficking resulting in complete regression of established murine tumors. PLoS One. 2013;8(3):e58860.

Talabostat mesylate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.12mL

3.22mL

1.61mL

32.24mL

6.45mL

3.22mL

Talabostat mesylate 技术信息

CAS号	150080-09-4
分子式	C₁₀H₂₃BN₂O₆S
分子量	310.17

别名	PT100 mesylate;Val-boroPro mesylate;Talabostat (mesylate);Val-boroPro;PT-100;Talabostat
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 40 mg/mL(128.96 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 250 mg/mL(806 mM)，配合低频超声助溶

动物实验配方

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00489710	Kidney Cancer	Phase 2	Withdrawn(Terminated for safet... 展开 >>y reasons) 收起 <<	-	-
NCT02083120	Pulmonary Disease, Chronic Obs... 展开 >>tructive 收起 <<	Not Applicable	Active, not recruiting	November 2018	Germany ... 展开 >> Helios Klinik Ambrock Hagen, NRW, Germany, 58091 收起 <<
NCT00083239	Melanoma Skin... 展开 >> Cancer 收起 <<	Phase 2	Completed	-	United States, Georgia ... 展开 >> Emory University/Winship Cancer Institute Atlanta, Georgia, United States, 30322-1013 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109-0473 United States, New Hampshire Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756-0001 United States, Pennsylvania University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213-2582 United States, Texas Mary Crowley Medical Research Center Dallas, Texas, United States, 75246 收起 <<
NCT00080080	Lung Cancer	Phase 2	Completed	-	United States, Florida ... 展开 >> Cancer Center of Florida Ocoee, Florida, United States, 34761 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Michigan Van Elslander Cancer Center Grosse Pointe Woods, Michigan, United States, 48236 United States, New York New York Oncology/Hematology--Albany Regional Cancer Center Albany, New York, United States, 12208 Mt. Sinai School of Medicine New York, New York, United States, 10029 USB Cancer Center-- Nyack Hospital Nyack, New York, United States, 10960 United States, Ohio Dayton Oncology & Hematology Kettering, Ohio, United States, 45409 United States, Texas Mary Crowley Medical Research Center Dallas, Texas, United States, 75246 Tyler Cancer Center Tyler, Texas, United States, 75702 United States, Washington Cancer Care Northwest Spokane, Washington, United States, 99218 收起 <<
NCT00083252	Melanoma Skin... 展开 >> Cancer 收起 <<	Phase 2	Completed	-	United States, Arkansas ... 展开 >> University of Arkansas Medical Sciences Little Rock, Arkansas, United States, 72205 United States, California Cancer Institute Medical Group, Inc. Santa Monica, California, United States, 90404 United States, Colorado University of Colorado Health Sciences Center Aurora, Colorado, United States, 80045 United States, Florida Cancer Center of Florida Ocoee, Florida, United States, 34761 United States, Indiana Indiana Hematology Oncology Consultants Indianapolis, Indiana, United States, 46202 United States, New Mexico New Mexico Cancer Center Alliance Albuquerque, New Mexico, United States, 87106 United States, New York NYU School of Medicine New York, New York, United States, 10016 Fifth Avenue Medical Healthcare New York, New York, United States, 10128 United States, North Carolina Carolinas Medical Center Charlotte, North Carolina, United States, 28203 United States, South Carolina Cancer Center of the Carolinas Greenville, South Carolina, United States, 29615 United States, Texas Mary Crowley Medical Research Center Dallas, Texas, United States, 75246 Tyler Cancer Center Tyler, Texas, United States, 75702 United States, Washington Cancer Care Northwest Research Spokane, Washington, United States, 99218 收起 <<
NCT00086203	Chronic Lymphocytic Leukemia	Phase 2	Completed	-	United States, Arkansas ... 展开 >> University of Arkansas for Medical Science Little Rock, Arkansas, United States, 72205 United States, Florida Ocala Oncology Center Ocala, Florida, United States, 34474 Gulfcoast Oncology Associates St. Petersburg, Florida, United States, 33705 United States, Indiana Indiana Oncology/Hematology Consultants Indianapolis, Indiana, United States, 46202 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Montana Hematology/Oncology Centers of the Northern Rockies Billings, Montana, United States, 59101 United States, Nevada Nevada Cancer Institute Las Vegas, Nevada, United States, 89135 United States, New York Queens Medical Associates, PC Fresh Meadows, New York, United States, 11365 Long Island Jewish Medical Center New Hyde Park, New York, United States, 11040 NYU Medical Center New York, New York, United States, 10016 James P. Wilmot Cancer Center/University of Rochester Rochester, New York, United States, 14642 United States, North Carolina Raleigh Hematology/Oncology Clinic Cary, North Carolina, United States, 27511 Wake Forest University Health Sciences Winston-Salem, North Carolina, United States, 27157 United States, Oklahoma Cancer Care Associates/Oklahoma City Oklahoma City, Oklahoma, United States, 73112 Cancer Care Associates--Tulsa Tulsa, Oklahoma, United States, 74136 United States, South Carolina Cancer Centers of the Carolinas Seneca, South Carolina, United States, 29672 United States, Texas Texas Cancer Center/Abilene Abilene, Texas, United States, 79606-5208 MD Anderson Cancer Center Houston, Texas, United States, 77030 United States, Virginia Virginia Oncology Associates-Lake Wright Cancer Center Norfolk, Virginia, United States, 23502 收起 <<
NCT00116389	Pancreatic Cancer ... 展开 >> Neoplasm Metastasis Adenocarcinoma 收起 <<	Phase 2	Terminated(FDA Hold May 2007)	-	-
NCT00243204	Carcinoma, Non-Small Cell Lung	Phase 3	Terminated(FDA Hold May 2007)	-	-
NCT00303940	Brain and Central Nervous Syst... 展开 >>em Tumors Childhood Germ Cell Tumor Kidney Cancer Liver Cancer Neuroblastoma Ovarian Cancer Sarcoma Unspecified Childhood Solid Tumor, Protocol Specific 收起 <<	Phase 1	Completed	-	United States, Maryland ... 展开 >> Warren Grant Magnuson Clinical Center - NCI Clinical Trials Referral Office Bethesda, Maryland, United States, 20892-1182 收起 <<

Talabostat mesylate {[allProObj[0].p_purity_real_show]}

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Talabostat mesylate 质控信息

Talabostat mesylate 生物活性

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Talabostat mesylate 技术信息

最近浏览的产品

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摩尔计算器

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总药量计算器

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细胞研究

临床研究

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Talabostat mesylate 纯度/质量文件产品仅供科研