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FK-448 Free base

MCE 国际站：FK-448 Free base

品牌：MedChemExpress (MCE)

货号：HY-100193

CAS 号：85858⁻⁷6-0

生物活性： FK-448 游离碱是胰凝乳蛋白酶的有效特异性抑制剂，IC50 为 720 nM。

体外研究(In Vitro)：FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM. FK-448 Free base slightly inhibits esterolysis of Trypsin and Thrombin, with IC50s of 780 and 35 µM, respectively, but shows no effects on esterolysis of plasmin, plasma kallikrein or pancreas kallikrein, with IC50s of all >1 mM[1]. FK-448 moderately inhibits hydrolytic activities of cathepsin G with an IC50 of 15 µM[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：FK-448 (20 mg/kg, i.p.) results in a decrease in the blood glucose level, and inhibits the degradation of insulin by pancreatic enzymes in rats. FK-448 (20 mg/kg, p.o.) also decreases the blood glucose level, and increases plasma IRI level in dogs[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：406.52

Formula：C25H30N2O3

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：请按照分析证书中推荐的条件储存产品。

Kinase Assay [1]：在底物浓度为 10 mM 的条件下，测定了胰蛋白酶 (0.5 µg/mL)、纤溶酶 (0.1 U/mL)、血浆激肽释放酶 (0.9 U/mL)、胰激肽释放酶 (4 U/mL) 和凝血酶 (6 U/mL) 对 TAME 的水解速率，以及胰凝乳蛋白酶 (2 µg/mL) 对 ATEE 的水解速率。同时测定了胰凝乳蛋白酶的酪蛋白水解活性。酪蛋白的最终浓度为 1%。为了测定抑制作用，将酶溶液和抑制剂的混合物在 37°C 下预孵育 10 分钟，然后测定残余酶活性。测定了 Km 和 Ki 值[1]。MCE 尚未独立确认这些方法的准确性。仅供参考。

Animal Administration [2]：Rats[2] Rats are anaesthetized with ethylcarbamate (0.9 g/kg, intraperitoneally), and a front midline incision is made to expose the viscera. A hypodermic needle attached to a syringe containing the test solution is then carefully inserted into the lumen of the jejunum 2cm under the pylons. Insulin is dissolved in saline (and 0.1 M HCl if necessary) and injected at 2 mL/kg. Although most inhibitors tested are soluble in water, chymostatin is insoluble, and so it is dissolved in DMSO (final concentration, 10%). For measurement of blood glucose, samples of 0.2 mL of blood are drawn from the inferior vena cava of rats before, and 1 h after treatment or before, 0.5, 1, 1.5,2, 3 and 4 h after that, and are centrifuged at 3000 rev/min for 10 min. The plasma glucose concentration of samples is determined, and indicated as relative percents of the blood glucose level at each period compared with that before administration (as 100%). Dogs[2] Enteric-coated gelatin capsules containing insulin and FK-448 are administered orally to the dogs and samples of 1 mL of blood are drawn from the median cubital vein before, and 0.5, 1, 1.5, 2, 2.5, 3, 4 and 5 h after treatment, are centrifuged at 3000 rev/min for 10min. The plasma glucose concentration of samples is also determined and indicated. Plasma IRI level is determined by double antibody radioimmunoassay using the Insulin-RIA kit[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

提供质量检测报告：Data Sheet、产品使用指南

产品活性：FK-448 Free base 是一种有效的，特异性的糜蛋白酶 (chymotrypsin) 抑制剂，IC50 值为 720 nM。

IC50 & Target：IC50: 720 nM (Chymotrypsin)[1]

相关产品：Bortezomib | PD150606 | Bortezomib (Standard) | Calpeptin | Carfilzomib | Carfilzomib (Standard) | Ixazomib | Alicapistat | KZR-504 | Ixazomib citrate | RA190 | Delanzomib

热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类

Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides

参考文献：
[1]. Fujii S, et al. New synthetic inhibitors of chymotrypsin. J Biochem. 1984 Feb;95(2):319-22.
[2]. Fujii S, et al. Promoting effect of the new chymotrypsin inhibitor FK-448 on the intestinal absorption of insulin in rats and dogs. J Pharm Pharmacol. 1985 Aug;37(8):545-9.