JTT551是一种选择性的蛋白酪氨酸磷酸酶1B(PTP1B)抑制剂，Ki值为0.22μM，同时对T细胞蛋白酪氨酸磷酸酶(TCPTP）也有作用，Ki值为9.3μM，可用于二型糖尿病的研究。
JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively. JTT 551 shows low affinity at CD45 PTP (CD45) and leucocyte common antigen-related (LAR) PTP with Kis of both >30 μM. Furthermore, JTT-551 (10 and 30 μM) enhances the insulin-induced deoxyglucose uptake in a dosedependent manner[1].
JTT 551 (3 mg/kg, 30 mg/kg, p.o.) dose-dependently decreases blood glucose level on Days 7, 14 and 28 in db/db Mice. JTT 551 also significantly reduces triglyceride (TG) level at 30 mg/kg on Day 7 but does not alter insulin and total cholesterol (TC) levels[1].
[1]. Fukuda S, et al. Pharmacological profiles of a novel protein tyrosine phosphatase 1B inhibitor, JTT-551. Diabetes Obes Metab. 2010 Apr;12(4):299-306.
Animal experiment: | Mice[1]Db/db mice are used in the assay. JTT 551 at doses of 3 or 30 mg/kg or pioglitazone at 3 mg/kg is administered orally to 6-week-old male db/db mice (n = 5) once daily for 4 weeks. Body weight is measured twice weekly and blood samples are collected from the orbital venous plexus before dosing on Days 7, 14 and 28. Blood glucose, insulin, triglyceride (TG) and total cholesterol (TC) levels are determined at the respective blood-sampling time points, and the haemoglobin A1c (HbA1c) level is determined before dosing on Day 28. HbA1c level is measured[1]. |
参考文献: [1]. Fukuda S, et al. Pharmacological profiles of a novel protein tyrosine phosphatase 1B inhibitor, JTT-551. Diabetes Obes Metab. 2010 Apr;12(4):299-306. | |
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