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PTP1B/AKR1B1-IN-1
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Catalog No. T78702
PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1].
PTP1B/AKR1B1-IN-1
PTP1B/AKR1B1-IN-1
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Catalog No. T78702
PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
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Storage & Solubility Information
| Description | PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1]. |
| In vitro | PTP1B/AKR1B1-IN-1 exhibits tight binding affinity to PTP1B and AKR1B1 with K_i values of 4.6 μM and 0.08 μM, respectively. At 20 μM for 24 hours, this compound shows negligible cytotoxicity in differentiated murine C2C12 myoblasts [1]. It also enhances insulin (10 μM, 15 minutes)-stimulated Akt phosphorylation in the C2C12 cell line at the same concentration and duration [1]. Additionally, PTP1B/AKR1B1-IN-1 (2 μM, 24 hours) significantly reduces sorbitol accumulation in the human lens epithelial cell line B3 (HLE) when co-incubated with 75 mM D-glucose for 24 hours [1]. |
| Molecular Weight | 427.54 |
| Formula | C22H21NO4S2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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 stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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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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