S83492 |
Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) |
| 源叶(MedMol) | 98% |
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- 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)
- 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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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
