Talabostat mesylate (Val-boroP

Talabostat mesylate  (Synonyms: Val-boroPro mesylate; PT100 mesylate)

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) 的第一个临床抑制剂 (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 。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
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生物活性    
Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (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    
DPP-4

体外研究
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[3].
? 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[4].

体内研究
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[4].

分子量    
310.18

性状    
Solid

Formula    
C10H23BN2O6S

CAS 号    
150080-09-4

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据    
In Vitro: 
H2O : 250 mg/mL (805.98 mM; Need ultrasonic)

DMSO : ≥ 40 mg/mL (128.96 mM)

* "≥" means soluble, but saturation unknown.

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    3.2239 mL    16.1197 mL    32.2393 mL
5 mM    0.6448 mL    3.2239 mL    6.4479 mL
10 mM    0.3224 mL    1.6120 mL    3.2239 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS

Solubility: 100 mg/mL (322.39 mM); Clear solution; Need ultrasonic

2.
请依序添加每种溶剂： Saline

Solubility: 50 mg/mL (161.20 mM); Clear solution; Need ultrasonic

3.
请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

4.
请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

5.
请依序添加每种溶剂： 10% DMSO    90% corn oil

Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution
 

参考文献

[1]. Lankas GR, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005 Oct;54(10):2988-94.  [Content Brief] [2]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13.  [Content Brief] [3]. Talabostat [4]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80.  [Content Brief]