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Talabostat mesylate (Synonyms: Val-boroPro mesylate; PT100 mesylate)
目录号: PC15727 纯度: ≥98%
CAS No. :150080-09-4
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PC15727-10mg 10mg ¥1744.40 请登录
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PC15727-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥1920.80 请登录
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中文名称
Talabostat mesylate
中文别名
Talabostat 甲磺酸盐;[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸甲磺酸盐;Talabostat mesilate 抑制剂;甲磺酸盐;噻帕西酮;甲基磺酸((R)-1-((S)-2-氨基-3-甲基丁酰)吡咯烷-2-基)硼酸(1:1)
英文名称
Talabostat mesylate
英文别名
Methanesulfonic acid ((R)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid (1:1);[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate;[(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid,methanesulfonic acid;Methanesulfonic acid ((R)-1-((S)-2-amino-3-methyl-butanoyl)pyrrolidin-2-yl)boronic acid (1:1);Talabostat-mesylate;PT100;PT-100;Talabostat mesylate;Talabostat mesylate (USAN);ValboroPro;Val-boroPro;Unii-V8zg4Y1B51;Talabostat Mesilate;[(2R)-1-(L-Valyl)-2-pyrrolidinyl]boronic acid methanesulfonate (1:1);Boronic acid, ((2R)-1-((2S)-2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)-, monomethanesulfonate;Talabostat mesylate [(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate;[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Talabostat mesilate;Talabostat (mesylate);Talabostat mesylate [USAN];V8ZG4Y1B51;PubChem18264;((2R)-1-((2S)-2-amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid me
Cas No.
150080-09-4
分子式
BC10N2O6SH23
分子量
310.18
包装储存

4°C, sealed storage, away from moisture

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

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.

性状

Solid

IC50 & Target[1][2]

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(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

H2O : 250 mg/mL (805.98 mM; Need ultrasonic)

DMSO : ≥ 40 mg/mL (128.96 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: PBS

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

  • 2.

    建议依照次序添加每种溶剂: Saline

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

  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    此方案可获得 ≥ 2.5 mg/mL (8.06 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

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

    此方案可获得 ≥ 2.5 mg/mL (8.06 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 5.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

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

    此方案可获得 ≥ 2.5 mg/mL (8.06 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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