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cis-THSG

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Catalog No. TN13934 Copy Product Info
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cis-THSG is an orally active and selective inhibitor of DNA topoisomerase II (DNAtopoisomeraseII), with no inhibitory activity against DNA topoisomerase I. It can inhibit the transcriptional expression of phosphoenolpyruvate carboxykinase (PEPCK). cis-THSG lowers blood glucose levels in male CF-1 mice with diet-induced diabetes, improves glucose intolerance, and alleviates insulin resistance. It is applicable in research related to type 2 diabetes.

cis-THSG

Cas No. 928205-59-8
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For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Bioactivity
Description
cis-THSG is an orally active and selective inhibitor of DNA topoisomerase II (DNAtopoisomeraseII), with no inhibitory activity against DNA topoisomerase I. It can inhibit the transcriptional expression of phosphoenolpyruvate carboxykinase (PEPCK). cis-THSG lowers blood glucose levels in male CF-1 mice with diet-induced diabetes, improves glucose intolerance, and alleviates insulin resistance. It is applicable in research related to type 2 diabetes.
In vitro
cis-THSG at a concentration of 100 μM for 30 minutes shows weak inhibitory activity against human DNA topoisomerase II, achieving an inhibition rate of 46% at this concentration, and exhibits no activity against DNA topoisomerase I. cis-THSG is not cytotoxic to HT-29, MCF-7, and HepG2 cell lines. At concentrations ranging from 30 to 100 μM over 8 hours, cis-THSG can inhibit the induction of PEPCK mRNA expression by Dexamethasone/8-CTP-cAMP in HepG2 cells, with the strongest inhibition (a 61.7% reduction in expression) observed at 30 μM after 8 hours.
In vivo
Cis-THSG (Drinking water contains 0.01%; freely available; daily; 12 weeks) demonstrates potent antidiabetic activity in HFD-induced male CF-1 diabetic mice. It significantly reduces hyperglycemia, hyperinsulinemia, and insulin resistance, and markedly improves impaired glucose tolerance.
Chemical Properties
Molecular Weight406.38
FormulaC20H22O9
Cas No.928205-59-8
SmilesO(C1=C(/C=C\C2=CC=C(O)C=C2)C=C(O)C=C1O)[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 µL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Related Tags: cis-THSG in vivo | cis-THSG in vitro | cis-THSG formula | cis-THSG molecular weight