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JTT 551

カタログ番号GC31499

JTT 551 は選択的なプロテイン チロシン ホスファターゼ 1B (PTP1B) 阻害剤であり、Kis は PTP1B および TCPTP (T 細胞プロテイン チロシン ホスファターゼ) に対してそれぞれ 0.22 μM および 9.3 μM です。 JTT 551 は、2 型糖尿病の研究に使用できます。

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JTT 551 化学構造

Cas No.: 776309-04-7

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Sample solution is provided at 25 µL, 10mM.

Description of JTT 551

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.

Protocol of JTT 551

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.

Chemical Properties of JTT 551

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
Formula C34H43N3O3S2 M.Wt 605.85
溶解度 DMSO : 100 mg/mL (165.06 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of JTT 551

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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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