Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) 98%

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate

源叶(MedMol)
S83492
150080-09-4
C10H23BN2O6S
310.175
[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸甲磺酸盐;TALABOSTAT 甲磺酸盐;甲基磺酸((R)-1-((S)-2-氨基-3-甲基丁酰)吡咯烷-2-基)硼酸(1:1);[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate;Talabostat mesylate;B
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S83492-5mg 98% ¥646.00元 7 - - -
源叶(MedMol) S83492-10mg 98% ¥900.00元 2 - - -
源叶(MedMol) S83492-50mg 98% ¥2550.00元 7 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) 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
产品描述: Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) 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
靶点: IC50: < 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP) Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9);Proteasome; DPP-4
体内研究: Talabostat mesylate (Val-boroPro mesylate) 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 mesylate (Val-boroPro mesylate) causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat mesylate (Val-boroPro mesylate) 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
参考文献: 1. Lankas GR, 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 Oct;54(10):2988-94. 2. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. 3. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80.
溶解性: H2O  :  250  mg/mL  (805.98  mM;  Need  ultrasonic)    DMSO  :  ≥  40  mg/mL  (128.96  mM)
保存条件: 2-8℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.224 ml 16.12 ml 32.24 ml
5 mM 0.645 ml 3.224 ml 6.448 ml
10 mM 0.322 ml 1.612 ml 3.224 ml
50 mM 0.064 ml 0.322 ml 0.645 ml
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参考文献

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