规格 | 价格 | 库存 | 数量 |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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靶点 |
DPP-4
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体外研究 (In Vitro) |
Talabostat 是一种非选择性 DPP-IV 抑制剂,抑制 DPP8/9、FAP、DPP2 和其他一些 DASH 家族酶的效果与抑制 DPP-IV 的效果基本相同[1]。 Talabostat 通过触发单核细胞和巨噬细胞中促炎性细胞死亡(称为细胞焦亡)来刺激免疫系统。两种丝氨酸蛋白酶 DPP8 和 DPP9 的抑制可激活 caspase-1 的前蛋白形式,不依赖于炎症小体接头 ASC[2]。 Talabostat竞争性抑制FAP和CD26/DPP-IV的二肽基肽酶(DPP)活性,并且由于Ser630/624与talabostat的硼之间形成复合物,与催化位点存在高亲和力相互作用[3] 。
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体内研究 (In Vivo) |
Talabostat 可以刺激针对肿瘤的免疫反应,涉及免疫系统的先天性和适应性分支。在 WEHI 164 纤维肉瘤以及 EL4 和 A20/2J 淋巴瘤模型中,PT-100 导致肿瘤消退和排斥。抗肿瘤作用似乎涉及肿瘤特异性 CTL 和保护性免疫记忆。 Talabostat 治疗接种 WEHI 164 的小鼠会增加细胞因子和趋化因子的 mRNA 表达,已知这些细胞因子和趋化因子可促进 T 细胞启动以及 T 细胞和先天效应细胞的化学吸引[3]。 Talabostat 治疗的小鼠纤维化明显减少,FAP 表达减少。 PT100 治疗后,还观察到肺部 MMP-12、MIP-1α 和 MCP-3 mRNA 表达水平的显着差异。在这种肺纤维化小鼠模型中使用 PT100 治疗具有抗纤维增殖作用并增加巨噬细胞活化[4]。
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动物实验 |
Mice: BLM (0.5mg/kg/day) is injected into male mice's nostrils on days -7, -6, -5, -2, -1, and 0. From day 1 to day 14, talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed twice a day. MRIs are done on days 0, 7, and 14 as well as prior to BLM. The animals are put to sleep after the final MRI scan, and their lungs are taken out for histology and quantitative real-time polymerase chain reaction (qRT-PCR) analysis[4].
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参考文献 |
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分子式 |
C10H23BN2O6S
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分子量 |
310.17
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精确质量 |
214.15
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元素分析 |
C, 50.50; H, 8.95; B, 5.05; N, 13.09; O, 22.42
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CAS号 |
150080-09-4
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相关CAS号 |
Talabostat isomer mesylate;Talabostat;149682-77-9
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外观&性状 |
Solid powder
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SMILES |
B([C@@H]1CCCN1C(=O)[C@H](C(C)C)N)(O)O.CS(=O)(=O)O
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InChi Key |
OXYYOEIGQRXGPI-WSZWBAFRSA-N
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InChi Code |
InChI=1S/C9H19BN2O3.CH4O3S/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15;1-5(2,3)4/h6-8,14-15H,3-5,11H2,1-2H3;1H3,(H,2,3,4)/t7-,8-;/m0./s1
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化学名 |
[(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid;methanesulfonic acid
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别名 |
Talabostat; BXCL701; BXCL-701; BXCL 701; Val-boro-pro; PT-100; PT100, PT 100; D05989
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
H2O: ~250 mg/mL (~806 mM)
DMSO: ≥ 40 mg/mL (~129 mM) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (322.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 5: 50 mg/mL (161.20 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2240 mL | 16.1202 mL | 32.2404 mL | |
5 mM | 0.6448 mL | 3.2240 mL | 6.4481 mL | |
10 mM | 0.3224 mL | 1.6120 mL | 3.2240 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04171219 | Active Recruiting |
Biological: Pembrolizumab Drug: Talabostat Mesylate |
Advanced Malignant Solid Neoplasm Recurrent Malignant Solid Neoplasm |
M.D. Anderson Cancer Center | March 19, 2020 | Phase 2 |
NCT00303940 | Completed | Drug: carboplatin Drug: talabostat mesylate |
Kidney Cancer Liver Cancer |
National Institutes of Health Clinical Center (CC) |
December 2005 | Phase 1 |