您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Talabostat
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Talabostat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Talabostat图片
CAS NO:149682-77-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
Val-boroPro
PT100
产品介绍
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 。
生物活性

Talabostat (Val-boroPro; PT100) is an orally active and nonselectivedipeptidyl peptidaseIV (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[1][2][3].

IC50& Target

IC50:< 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP)[1]
Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9)[2]

体外研究
(In Vitro)

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[3].
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[4].

体内研究
(In Vivo)

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[4].

Clinical Trial
分子量

214.07

Formula

C9H19BN2O3

CAS 号

149682-77-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vitro: 

DMSO : ≥ 40 mg/mL(186.85 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.6714 mL23.3568 mL46.7137 mL
5 mM0.9343 mL4.6714 mL9.3427 mL
10 mM0.4671 mL2.3357 mL4.6714 mL