中文名 | [(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸 |
英文名 | VAL-BORO-PRO |
别名 | [(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸 |
英文别名 | Pt 100 talabostat VAL-BORO-PRO Unii-kz1o2sh88z Talabostat (PT100) [(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid Boronic acid, ((2R)-1-((2S)-2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)- Boronic acid, (1-(2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)-, (R-(R*,S*))- |
CAS | 149682-77-9 |
化学式 | C9H19BN2O3 |
分子量 | 214.07 |
InChI | InChI=1/C9H19BN2O3/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15/h6-8,14-15H,3-5,11H2,1-2H3/t7-,8-/m0/s1 |
密度 | 1.15 |
沸点 | 421.4±55.0 °C(Predicted) |
酸度系数 | 9.71±0.20(Predicted) |
存储条件 | Room Temprature |
体外研究 | By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat (Val-boroPro) inhibits dipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity. Talabostat (Val-boroPro) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site. |
体内研究 | Talabostat (Val-boroPro; PT100) 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 (Val-boroPro) causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory.Talabostat (Val-boroPro) 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. |
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