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Purity: ≥98%
PTP1B-IN-2 is a potent and selective protein tyrosine phosphatase-1B (PTP1B) inhibitor. PTP1B as a key negative regulator of both insulin and leptin receptor pathways has been an attractive therapeutic target for the treatment of type 2 diabetes mellitus (T2DM) and obesity. With the goal of enhancing potency and selectivity of the PTP1B inhibitors, a series of methyl salicylate derivatives as ABC type PTP1B inhibitors (P1-P7) were discovered. More importantly, compound P6 (PTP1B-IN-2) exhibited high potent inhibitory activity (IC50 = 50 nM) for PTP1B with 15-fold selectivity over T-cell PTPase (TCPTP). Further studies on cellular activities revealed that PTP1B-IN-2 could enhance insulin-mediated insulin receptor β (IRβ) phosphorylation and insulin-stimulated glucose uptake.
| ln Vitro |
PTP1B-IN-2 exhibits a selectivity for PTP1B that is over 40 times greater than that of SHP-2 and LAR, and 15 times greater than that of the highly homologous TCPTP. PTP1B-IN-2 reaches far into the active site pocket, where it interacts hydrophobically and forms several hydrogen bonds with important catalytic residues. The binding characteristics of the PTP1B domain and ligands indicate that PTP1B-IN-2 is an ABC-type inhibitor that interacts not only with the catalytic site, but also with the B site and C site. PTP1B-IN-2 greatly enhances insulin-mediated IRβ phosphorylation at concentrations of 15 μM and 30 μM. L6 myotubes treated with PTP1B-IN-2 also showed a significant increase in insulin-stimulated glucose uptake, with increases of 16.0%, 19.0%, and 38.1% at 5, 10, and 20 μM, respectively [1].
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| References |
[1]. Liu P, et al. Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity. Eur J Med Chem. 2016 Aug 8;118:27-33
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| Molecular Formula |
C34H36N2O9S2
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| Molecular Weight |
680.78
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| CAS # |
1919853-46-5
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| Related CAS # |
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| SMILES |
O=S(N(CC1=CC=C(C=C1)N(CC(OC)=O)S(C)(=O)=O)C(C=C2)=CC=C2OCC3=CC(C(OC)=O)=C(C)C=C3)(CC4=CC=CC=C4)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4689 mL | 7.3445 mL | 14.6890 mL | |
| 5 mM | 0.2938 mL | 1.4689 mL | 2.9378 mL | |
| 10 mM | 0.1469 mL | 0.7345 mL | 1.4689 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Eur J Med Chem.2016 Aug 8;118:27-33. |
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Eur J Med Chem.2016 Aug 8;118:27-33. |
Eur J Med Chem.2016 Aug 8;118:27-33. |
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