Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LMPTP INHIBITOR 1 hydrochloride 是一种高选择性的低分子量蛋白酪氨酸磷酸酶 (LMPTP) 抑制剂。LMPTP INHIBITOR 1 (hydrochloride) 能够抑制 LMPTP-A 的活性,IC50值为 0.8 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,780 | 现货 | ||
5 mg | ¥ 4,480 | 现货 | ||
10 mg | ¥ 6,380 | 现货 | ||
25 mg | ¥ 9,620 | 现货 | ||
50 mg | ¥ 12,900 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,990 | 现货 |
产品描述 | LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase ( LMPTP ), with an IC 50 of 0.8 μM for LMPTP-A. |
靶点活性 | LMPTPA:0.8 μM |
体外活性 | LMPTP INHIBITOR 1 (hydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase, with an IC 50 of 0.8 μM for LMPTP-A. LMPTP INHIBITOR 1 shows more potent effect on LMPTP-A versus LMPTP-B. LMPTP inhibitor 1 (Compound 23; 10 μM) also enhances HepG2 IR phosphorylation after insulin stimulation in human HepG2 hepatocytes [1]. |
体内活性 | LMPTP inhibitor 1 is orally bioavailable, and results in appr 680 nM mean serum concentration after treatment of 0.03% w/w, while treatment with 0.05% w/w results in >3 μM; which also reverses diabetes in obese mice. LMPTP inhibitor 1 (0.05% w/w) inhibits LMPTP activity, significantly improves glucose tolerance and reduces fasting insulin levels of diabetic DIO mice, without affecting body weight [1]. |
激酶实验 | Phosphatase assays are performed in buffer containing 50 mM Bis-Tris, pH 6.0, 1 mM DTT and 0.01% Triton X-100 at 37°C. For assays conducted with 3-O-methylfluorescein phosphate (OMFP) as substrate, fluorescence is monitored continuously at λex = 485 and λem = 525 nm. For assays conducted with para-nitrophenyl phosphate (pNPP) as substrate, the reaction is stopped by addition of 2X reaction volume of 1 M NaOH, and absorbance is measured at 405 nm. IC50 values are determined from plots of LMPTP inhibitor 1 concentration versus percentage of enzyme activity. For inhibitor selectivity assays, each PTP is incubated with either 0.4 mM OMFP or 5 mM pNPP in the presence of 40 μM LMPTP inhibitor 1 or DMSO. Equal units of enzyme activity, comparable to the activity of 10 nM human LMPTP-A, are used. For the inhibitor reversibility assay, 50 nM human LMPTP-A is pre-incubated with 10 μM LMPTP inhibitor 1 or DMSO for 5 min. The enzyme is diluted 100X in phosphatase assay buffer containing 0.4 mM OMFP and fluorescence is measured at the indicated time points [1]. |
细胞实验 | Human HepG2 cells are cultured in Eagle's Minimal Essential Medium (ATCC) containing 10% fetal bovine serum (FBS), 100 U/mL penicillin and 100 μg/mL streptomycin. The absence of Mycoplasma contamination in HepG2 cultures is confirmed using the Lonza MycoAlert Mycoplasma Detection Kit. Cells are treated with 10 μM LMPTP inhibitor 1 in serum-starvation media (0.1% FBS) overnight, following which cells are stimulated with 10 nM bovine insulin for 5 min at 37°C. For detection of IR tyrosine phosphorylation by immunoprecipitation/Western blotting, cells are lysed in radioimmunoprecipitation assay buffer containing 1 mM phenylmethylsulfonyl fluoride, 10 μg/mL aprotinin/leupeptin, 10 mM sodium orthovanadate, 5 mM sodium fluoride, and 2 mM sodium pyrophosphate, and the IR is immunoprecipitated using the anti-IRβ Ab. IR tyrosine phosphorylation of immunoprecipitates is determined by Western blotting with the anti-pIR/pIGFR-Y1162/Y1163 Ab [1]. |
动物实验 | LMPTP inhibitor 1 is administered to male B6 or Acp1fl/fl albumin-Cre+ DIO mice at 0.05% w/w in high-fat diet (HFD) rodent chow. Control groups consist of male B6 or Acp1fl/fl albumin-Cre+ littermate mice administered HFD rodent chow alone. Mice are allowed food and water ad libitum and weighed daily. Randomization is not used in these experiments; rather littermate mice are assigned to treatment or control groups in a manner to maintain similar mean body weights between the 2 groups at the start of the study. Insulin-induced liver IR phosphorylation, IPGTT, and fasting insulin levels are assessed after treatment. Diabetic (displaying overnight [13 hr] fasting blood glucose levels ≥140 mg/dL) B6 DIO mice are used in experiments to assess IPGTT and fasting insulin levels [1]. |
别名 | LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base)) |
分子量 | 481.07 |
分子式 | C28H37ClN4O |
CAS No. | 2310135-38-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9 mg/mL (18.71 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0787 mL | 10.3935 mL | 20.787 mL | 51.9675 mL |
5 mM | 0.4157 mL | 2.0787 mL | 4.1574 mL | 10.3935 mL | |
10 mM | 0.2079 mL | 1.0393 mL | 2.0787 mL | 5.1967 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。
LMPTP INHIBITOR 1 hydrochloride 2310135-38-5 Metabolism Phosphatase LMPTP INHIBITOR 1 Hydrochloride LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base)) Inhibitor inhibitor inhibit