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Talabostat mesylate

CAS No. : 150080-09-4

MCE 站：Talabostat mesylate

产品活性：Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) 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; K_i = 0.18 nM) 和成纤维细胞活化蛋白 (FAP) 的个临床抑制剂 (IC₅₀ = 560 nM)，抑制 DPP8/9 (IC₅₀ = 4/11 nM; K_i = 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 。

研究领域：Metabolic Enzyme/Protease

作用靶点：Dipeptidyl Peptidase

In Vitro: By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat mesylate (Val-boroPro mesylate) 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 mesylate (Val-boroPro mesylate) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site.

In Vivo: 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.

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