Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 931 | 待询 | ||
10 mg | ¥ 1,381 | 待询 | ||
50 mg | ¥ 5,269 | 待询 |
Talabostat 的其他形式现货产品:
产品描述 | Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. |
靶点活性 | DPP4:< 4 nM (IC50), DPP4:0.18 nM (Ki), DPP8/9:1.5/0.76 nM (Ki), DPP8/9:4/11 nM (IC50), QPP:310 nM (IC50), FAP:560 nM (IC50) |
体外活性 | Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat[3]. |
体内活性 | Talabostat 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, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat 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[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. |
分子量 | 214.07 |
分子式 | C9H19BN2O3 |
CAS No. | 149682-77-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: ≥ 40 mg/mL (186.85 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.6714 mL | 23.3568 mL | 46.7137 mL | 116.7842 mL |
5 mM | 0.9343 mL | 4.6714 mL | 9.3427 mL | 23.3568 mL | |
10 mM | 0.4671 mL | 2.3357 mL | 4.6714 mL | 11.6784 mL | |
20 mM | 0.2336 mL | 1.1678 mL | 2.3357 mL | 5.8392 mL | |
50 mM | 0.0934 mL | 0.4671 mL | 0.9343 mL | 2.3357 mL | |
100 mM | 0.0467 mL | 0.2336 mL | 0.4671 mL | 1.1678 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Talabostat 149682-77-9 Inhibitor inhibitor inhibit