149682-77-9

中文名称 [(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸

英文名称 VAL-BORO-PRO

CAS 149682-77-9

分子式 C9H19BN2O3

分子量 214.07

MOL 文件 149682-77-9.mol

149682-77-9 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

[(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
TALABOSTA
talabostat
VAL-BORO-PRO
Unii-kz1o2sh88z
Talabostat (PT100)
Talabostat (Val-boroPro, PT-100)
PT-100
VALBOROPRO
VAL-BOROPRO
PT100
PT 100
[(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid
[(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid

物理化学性质

沸点421.4±55.0 °C(Predicted)

密度1.15

储存条件-20°C储存

溶解度DMSO : ≥ 40 mg/mL (186.85 mM)

酸度系数(pKa)9.71±0.20(Predicted)

常见问题列表

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。

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.