[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸
![[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸,149682-77-9,结构式](https://www.chemicalbook.com/CAS/20180808/GIF/149682-77-9.gif)
- CAS号:149682-77-9
- 英文名:VAL-BORO-PRO
- 中文名:[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸
- CBNumber:CB01011676
- 分子式:C9H19BN2O3
- 分子量:214.07
- MOL File:149682-77-9.mol
- 沸点 :421.4±55.0 °C(Predicted)
- 密度 :1.15
- 储存条件 :Store at -20°C
- 溶解度 :DMSO : ≥ 40 mg/mL (186.85 mM)
- 酸度系数(pKa) :9.71±0.20(Predicted)
[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸性质、用途与生产工艺
- 生物活性 Talabostat (Val-boroPro; PT100) 是一种口服活性和非选择性的二肽基肽酶 IV (DPP-IV) 抑制剂 (IC50 < 4 nM; Ki = 0.18 nM) 和成纤维细胞活化蛋白 (FAP) 的第一个临床抑制剂 (IC50 = 560 nM)，抑制 DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM)，静息细胞脯氨酸二肽酶 (QPP) (IC50 = 310 nM)、DPP2 和一些其他 DASH 家族酶。具有抗肿瘤和造血刺激活性 。
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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.
- 公司名称：Qualy Chem
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- 国家：印度
- 产品数：7
- 优势度：58
