JTT 551
目录号 : GC31499JTT551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。
Cas No.:776309-04-7
Sample solution is provided at 25 µL, 10mM.
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]. |
References: [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. |
Cas No. | 776309-04-7 | SDF | |
Canonical SMILES | O=C(O)CN(CC1=NC=C(C(C)(C)C)S1)CC2=NC(C3=CC=C(COC4=CC=C(C(CCC)CCC)C=C4)C=C3)=CS2 | ||
分子式 | C34H43N3O3S2 | 分子量 | 605.85 |
溶解度 | DMSO : 100 mg/mL (165.06 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.6506 mL | 8.2529 mL | 16.5057 mL |
5 mM | 0.3301 mL | 1.6506 mL | 3.3011 mL |
10 mM | 0.1651 mL | 0.8253 mL | 1.6506 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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