| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
Preparation Method | Human kinases activities were measured using KINOMEscan. In brief, 256 DNA-tagged kinases, ligand affinity beads, and MSI-1436 (Trodusquemine)(10 ?mol/l) were incubated at room temperature, washed, and then eluted. Phage titer in the eluates was quantitated by real-time quantitative PCR. |
Reaction Conditions | 10 ?mol/l MSI-1436 (Trodusquemine) |
Applications | Enzyme inhibition assay showed that MSI-1436 (Trodusquemine) inhibited PTP1B 200 times more in a dose-dependent manner than TCPTP (IC 50 = 1 umol/l vs. 224 umol/l). |
Cell lines | HepG2 cell line |
Preparation Method | Hep G2 cells were pretreated with 10 ?mol/l MSI-1436 (Trodusquemine) or sodium orthovanadate for 10 min at 37 ℃, then incubated with 10 mmol/l pNPP for 30 min at 37 ℃. Samples of the supernatants were spectrophotometrically analyzed at OD405 for hydolyzed pNP, a direct end product of phosphatase activity. |
Reaction Conditions | 10 ?mol/l MSI-1436 (Trodusquemine) for 10 min at 37 ℃ |
Applications | Quantification of phosphatase activity measured in intact cell assays Incubation of intact HepG2 cells with 10 umol/l MSI-1436 (Trodusquemine) resulted in a 53% inhibition of phosphatase activity compared with control (no inhibitor). |
Animal models | Male AKR/J mice |
Preparation Method | Male AKR/J mice were randomly placed on ad libitum 10, 45, or 60% fat kcal diets.After 14 weeks, mice were randomly assigned to three treatment groups; MSI-1436 (Trodusquemine), vehicle, or pair-fed. PF animals were injected with saline and allotted the amount of food consumed daily by trodusquemine-treated animals. |
Dosage form | MSI-1436 (Trodusquemine)(initial dose of 10 mg/kg followed by intraperitoneal injection of 5 mg/kg 3 times weekly) for 23 days |
Applications | MSI-1436 (Trodusquemine)-treated animals demonstrated weight loss in a manner proportional to their pretreatment weights; heavier mice lost a greater overall percentage of BW. |
| 产品描述 | MSI-1436 (Trodusquemine) is a selective non-competitive inhibitor of the enzyme protein tyrosine phosphatase 1B (PTB1B). The IC50 of MSI-1436 is about 1 µM, which is 200 times higher than that of TCPTP (IC50, 224 µM).[1]. Besides,it has antimicrobial activity[6]. Incubation of intact HepG2 cells with 10µM MSI-1436 (Trodusquemine) resulted in a 53% inhibition of phosphatase activity compared with control (no inhibitor)[1]. MSI-1436 (Trodusquemine) is a "first-in-class" highly selective inhibitor of PTP1B that can cross the blood-brain barrier to suppress feeding and promote insulin sensitivity and glycemic control. in cultured neuronal cells[2]. Selective inhibition of PTP1B in equine ASC EMS cells improved substantially adipogenic differentiation by promoting cellular proliferation and normalizing expression of C/EBPalpha, PPARγ. Levels of secreted adiponectin and PPARγ were also shown to be increased in MSI-1436 (Trodusquemine)-conditioned cells, while total leptin levels markedly dropped under the same conditions[4]. MSI-1436 (Trodusquemine) acts rapidly and leads to significant weight loss after the first dose. A prerequisite for safe and effective antiobesity therapy is to reduce fat without reducing lean muscle mass Trodusquemine Treated mice had no reduction in whole-body protein content, but smaller epididymal fat pads, reduced adipocyte area in white and brown adipose tissue, and significant reduction in whole-body fat composition fat-specific non-cachexic weight loss in MSI-1436 (Trodusquemine) could explain the dependence of percentage weight loss on initial body weight[1]. A single injection of the drug MSI-1436 (Trodusquemine) decreased food intake in rats. To assess the effects of MSI-1436 (Trodusquemine) on DAT function, fast-scan cyclic voltammetry was used to measure DA concentration changes in the ventral striatum. Neither saline nor MSI-1436 (Trodusquemine) caused a significant change in the magnitude of evoked release from baseline values whereas bupropion caused a significant increase. MSI-1436 (Trodusquemine) as an anti-obesity treatment which spares DAT[5]. MSI-1436 (Trodusquemine) antagonized HER2 signaling, inhibited tumorigenesis in xenografts and abrogated metastasis in the NDL2 mouse model of breast cancer, validating inhibition of PTP1B as a therapeutic strategy in breast cancer[7]. The PTP1B inhibitor MSI-1436 (Trodusquemine) normalizes PTP1B activity, restores mGluR5 function, and attenuates the anxiety phenotype in LMO4 KO mice[3]. References: |
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