| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PTP1B-IN-22 selectively targets protein tyrosine phosphatase 1B (PTP1B), a member of the protein tyrosine phosphatase family that dephosphorylates the activated insulin receptor and its downstream substrates. By inhibiting PTP1B, the compound enhances insulin receptor signaling and improves glucose uptake in insulin-responsive tissues. PTP1B-IN-22 shows selectivity for PTP1B over other phosphatases. The compound's mechanism of action involves binding to the active site of PTP1B and preventing substrate dephosphorylation.
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| ln Vitro |
PTP1B-IN-22 (compound 3j; skeletal muscle L6 myotubes) demonstrates a 39.6% increase in glucose absorption in vitro and 66.4% inhibition of PTP1B [1].
In vitro, PTP1B-IN-22 demonstrates 66.4% inhibition of PTP1B enzyme activity. The compound also increases glucose uptake by 39.6% in skeletal muscle L6 myotubes. These findings demonstrate the compound's efficacy in enhancing insulin signaling and glucose metabolism in cellular models. PTP1B-IN-22 shows concentration-dependent inhibition of PTP1B activity in biochemical assays and promotes glucose uptake in insulin-responsive cells. |
| ln Vivo |
In vivo activity data for PTP1B-IN-22 are limited, as the compound is primarily studied in vitro. Based on its PTP1B inhibitory mechanism and glucose uptake-promoting activity, the compound is expected to improve glucose tolerance and insulin sensitivity in animal models of diabetes and obesity. However, detailed efficacy studies in animal models have not been extensively reported. The compound's potential for in vivo applications requires further investigation.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for PTP1B-IN-22 typically involves measuring PTP1B activity using a synthetic substrate such as p-nitrophenyl phosphate (pNPP) or a fluorogenic substrate. Purified recombinant human PTP1B enzyme is incubated with varying concentrations of PTP1B-IN-22 (0.01-100 µM) in assay buffer at 37°C for 10-15 minutes. The reaction is initiated by adding the substrate, and after incubation, the reaction is stopped. Absorbance or fluorescence is measured, and percent inhibition is calculated.
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| Cell Assay |
For in vitro cell-based assays, skeletal muscle L6 myotubes or other insulin-responsive cell lines are cultured and treated with PTP1B-IN-22 at concentrations ranging from 0.1-100 µM for 24-48 hours. Glucose uptake is measured using 2-deoxyglucose uptake assays with radiolabeled or fluorescent tracers. PTP1B activity is measured in cell lysates using a phosphatase activity assay kit. Insulin signaling is evaluated by Western blot analysis of phosphorylated insulin receptor and Akt.
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| Animal Protocol |
In vivo animal studies for PTP1B-IN-22 have not been extensively reported. Based on the compound's mechanism as a PTP1B inhibitor, potential in vivo studies would involve administration to diabetic or obese mouse models via oral gavage or intraperitoneal injection at doses ranging from 1-50 mg/kg. Efficacy would be assessed by measuring blood glucose levels, insulin sensitivity, and glucose tolerance. Tissue samples would be collected for analysis of PTP1B activity and insulin signaling biomarkers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PTP1B-IN-22 have not been fully characterized. Molecular formula is C₁₆H₁₂N₂O₃S₂. CAS number is 86109-60-6. Detailed pharmacokinetic parameters such as bioavailability, half-life, and protein binding have not been reported. Stability in solution may be limited and fresh solutions should be prepared for each experiment. The compound should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Toxicology data for PTP1B-IN-22 are limited. As a research compound, it has not been systematically evaluated for safety. The compound's mechanism of PTP1B inhibition suggests a generally favorable safety profile, but potential off-target effects and chronic toxicity remain to be evaluated. Standard toxicological endpoints including cell viability, genotoxicity, and organ toxicity should be evaluated. The compound is intended for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
PTP1B-IN-22 is a potent PTP1B inhibitor that demonstrates 66.4% enzyme inhibition and 39.6% increase in glucose uptake in skeletal muscle L6 myotubes. The compound is a valuable research tool for studying PTP1B function in insulin signaling, glucose metabolism, and metabolic diseases. PTP1B-IN-22 supports investigations into therapeutic strategies targeting PTP1B for diabetes and obesity. It is intended for research use only and is not approved for therapeutic use.
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| Molecular Formula |
C16H12N2O3S2
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|---|---|
| Molecular Weight |
344.41
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| Exact Mass |
344.028
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| CAS # |
86109-60-6
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| PubChem CID |
742352
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.741
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| LogP |
4.33
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
441
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)N=C(S2)SCC(=O)NC3=CC=C(C=C3)C(=O)O
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| InChi Key |
ARVQDURBWHSEPA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12N2O3S2/c19-14(17-11-7-5-10(6-8-11)15(20)21)9-22-16-18-12-3-1-2-4-13(12)23-16/h1-8H,9H2,(H,17,19)(H,20,21)
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| Chemical Name |
4-[[2-(1,3-benzothiazol-2-ylsulfanyl)acetyl]amino]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO: 100 mg/mL (290.35 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (7.26 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 | 2.9035 mL | 14.5176 mL | 29.0352 mL | |
| 5 mM | 0.5807 mL | 2.9035 mL | 5.8070 mL | |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9035 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.
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