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Ertiprotafib
🥰Excellent
Catalog No. T15243Cas No. 251303-04-5
Alias PTP-112, PTP112, PTP 112
Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.
Ertiprotafib
🥰Excellent
Purity: 98.70%
Catalog No. T15243Alias PTP-112, PTP112, PTP 112Cas No. 251303-04-5
Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $84 | In Stock | |
| 5 mg | $198 | In Stock | |
| 10 mg | $347 | In Stock | |
| 25 mg | $668 | In Stock | |
| 50 mg | $987 | In Stock | |
| 100 mg | $1,330 | In Stock |
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This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:98.70%
ee:100%
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Product Introduction
Bioactivity
Chemical Properties
| Description | Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer. |
| Targets&IC50 | PPARα:~1 μM (EC50), PTP1B:1.6 μM, PPARβ:~1 μM (EC50), IKKβ:400 nM |
| In vitro | METHODS: To measure the kinase activity of IKK-b, ertiprotafib was used in doses (0.001-1 μM) and a peptide substrate containing the IjB phosphorylation motif was used, and the phosphorylated peptide product was determined using an ELISA-type assay with time-resolved fluorescence (TRF) measurements. RESULTS: Ertiprotafib is a potent IKK-b inhibitor with an IC50 value of 400 ± 40 nM, which is well below the value required for half-maximal inhibition of PTP1B p-nitrophenyl phosphatase activity. The reported IC50 values of ertiprotafib for PTP1B range from 1.6 to 29 μM, depending on the assay conditions. [1] |
| In vivo | METHODS: Here, 11-week-old leptin-deficient male ob/ob mice were administered Ertiprotafib (25 mg/kg, daily, for 4 days), and changes in blood glucose indicators were observed. RESULTS: Mice treated with ertiprotafib had fasting blood glucose levels returned to the normal range, along with a significant decrease in insulin levels and a significant decrease in serum triglyceride levels. [2] |
| Synonyms | PTP-112, PTP112, PTP 112 |
| Molecular Weight | 559.51 |
| Formula | C31H27BrO3S |
| Cas No. | 251303-04-5 |
| Smiles | CC=1C2=C(C=3C(C(Br)=C2SC1C)=CC=CC3)C4=CC(C)=C(O[C@H](CC5=CC=CC=C5)C(O)=O)C(C)=C4 |
| Relative Density. | 1.376 g/cm3 (Predicted) |
| Color | Yellow |
| Appearance | Solid |
Storage & Solubility Information
| Storage | keep away from moisture,store under nitrogen,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (142.98 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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