1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETalabostat mesylateCat. No.: HY-13233ACAS No.: 150080-09-4Synonyms: Val-boroPro (mesylate); PT100 (mesylate)分式: CHBNOS分量: 310.18作靶點: Dipeptidyl Peptidase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent

2、-80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 40 mg/mL (128.96 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.2239 mL 16.1197 mL 32.2393 mL5 mM 0.6448 mL 3.2239 mL 6.4479 mL10 mM 0.3224 mL 1.6120 mL 3.2239 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實

3、驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結果的可靠性，體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.06 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8

4、.06 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.06 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Talabostat mesylate (Val-boroPro mesylate)種服活性和選擇性的肽基肽酶 IV (DPP-IV) 抑制劑 (IC50 4 nM; Ki = 0.18 nM) 和成纖維細胞活化蛋 (FAP) 的第個臨床抑制劑

5、(IC50 = 560 nM)，抑制 DPP8/9(IC50 = 4/11 nM; Ki = 1.5/0.76 nM)，靜息細胞脯氨酸肽酶 (QPP) (IC50 = 310 nM)、DPP2 和些其他 DASH家族酶。具有抗腫瘤和造刺激活性 1 2 3。IC50 & Target IC50: 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP) 1Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9) 2體外研究 By cleaving N-terminal Xaa-Pro or Xaa-Ala

6、residues, Talabostat mesylate (Val-boroPro mesylate) inhibitsdipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production andspecific T-cell immunity and T-cell dependent activity 3.Talabostat mesylate (Val-boroPro mesylate) competitively inhibits the dipepti

7、dyl peptidase (DPP) activity ofFAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site 4.體內研究 Talabostat mesylate (Val-boroPro mesylate) can stimulate immune responses against tumors involving boththe innate and adaptive branches of the immune system. In WEHI 164 fibros

8、arcoma and EL4 and A20/2Jlymphoma models, Talabostat mesylate (Val-boroPro mesylate) causes regression and rejection of tumors.The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostatmesylate (Val-boroPro mesylate) treatment of WEHI 164-inoculated mi

9、ce increases mRNA expression ofcytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innateeffector cells 4.PROTOCOLAnimal Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostrils of male mice. TalabostatAdministration 4 (40 g/mouse

10、) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed beforeBLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvestedfor histological and quantitative real-time polymerase chain reaction (qRT-PCR) analyses 4.MCE has not

11、 independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Nat Commun. 2019 May 7;10(1):2091. Cancer Res. 2016 Jul 15;76(14):4124-35. Anal Chem. 2016 Aug 16;88(16):8309-14. J Biol Chem. 2018 Dec 7;293(49):18864-18878. bioRxiv. Feb. 7, 2018.2/3 Master of Small Mol

12、ecules 您邊的抑制劑師www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lankas GR, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidylpeptidases 8 and 9. Diabetes. 2005 Oct;54(10):2988-94.2. Conno

13、lly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. JMed Chem. 2008 Oct 9;51(19):6005-13.3. Talabostat4. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediatedcytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80.Mc