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Talabostat mesylate

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Chemical Structure| 150080-09-4 同义名 : PT100 mesylate;Val-boroPro mesylate;Talabostat (mesylate);Val-boroPro;PT-100;Talabostat
CAS号 : 150080-09-4
货号 : A264157
分子式 : C10H23BN2O6S
纯度 : 99%+
分子量 : 310.17
MDL号 : MFCD13194906
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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 IC50 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].
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NCT00489710 Kidney Cancer Phase 2 Withdrawn(Terminated for safet...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 <<
实验方案
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
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.