WB403
Based on 1 Customer Validation
WB403 is an orally active TGR5 activator with an EC50 of 5.5 μM against human TGR5. WB403 activates TGR5 to stimulate downstream signaling pathways, promote GLP-1 secretion, improve glucose tolerance in mice with type 2 diabetes, and reduce levels of fasting blood glucose, postprandial blood glucose and HbA1c. WB403 increases pancreatic β-cell mass and restores the distribution of α-cells and β-cells in islets. WB403 is applicable to the research of type 2 diabetes.
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- Purity: 99.16%
- CAS No.: 1594041-84-5
- 화학식: C19H19BrN2OS
- 분자량:403.34
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
WB403 (1-20 μM; 16 h) dose-dependently activates human TGR5 in transiently transfected 293T cells with an EC50 of 5.5 μM, as measured by a CRE-luciferase reporter assay[1].
WB403 (10 μM; 30 min) significantly stimulates active GLP-1 secretion from human NCI-H716 enteroendocrine cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:293T cells (transiently transfected with pTGR5)
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Concentration:0, 1, 5, 10, 20, 50 μM
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Incubation Time:30 min
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Result:Dose-dependently stimulated TGR5-mediated cAMP accumulation, with statistically significant increases observed at all tested concentrations relative to the DMSO (+TGR5) control.
Showed no stimulation in control 293T cells transfected with an empty plasmid.
WB403 (50-100 mg/kg; p.o.; daily; for 4 consecutive weeks) significantly reduces fasting and postprandial blood glucose levels, decreases HbA1c, increases insulin levels, restores the normal distribution of islet cells, and expands islet area in spontaneous type 2 diabetic db/db mice[1].
WB403 (50-100 mg/kg; p.o.; single administration) significantly improves glucose tolerance and increases serum GLP-1 levels in normal ICR mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, 5 weeks old, high-fat diet + streptozotocin-induced type 2 diabetes)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 8 weeks
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Result:Significantly decreased fasting blood glucose and postprandial blood glucose starting from the first week of intervention, with effects sustained throughout the 8-week treatment period.
Significantly reduced serum HbA1c levels compared to vehicle controls.
Restored pancreatic islet area to near-normal levels, reversing β-cell loss induced by streptozotocin.
Decreased water intake, indicating improved hyperglycemia, while food intake and body weight did not vary significantly compared to vehicle controls.
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Animal Model:db/db (C57BL BKS cg-M+/+ lepr-/-) mice (male, 8 weeks old, spontaneous type 2 diabetes)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 4 weeks
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Result:Significantly decreased fasting blood glucose and postprandial blood glucose after 1 week of treatment, with effects sustained throughout the 4-week period.
Significantly reduced serum HbA1c levels and increased serum insulin levels compared to vehicle controls.
Decreased water intake, indicating improved hyperglycemia, while food intake and body weight did not vary significantly compared to vehicle controls.
Reduced α-cell infiltration in the islet core, restoring the normal distribution pattern of α-cells (peripheral) and β-cells (core), and increased pancreatic islet area compared to vehicle controls.
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Animal Model:ICR mice (male, non-diabetic)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o.; single dose; 30 minutes before glucose challenge
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Result:Significantly improved glucose tolerance in normal mice, as shown by reduced blood glucose levels during oral glucose tolerance test and decreased area under the curve (AUC) compared to vehicle controls.
Significantly increased serum GLP-1 concentrations compared to vehicle controls.
Chemical Information
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CAS No. 1594041-84-5
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Appearance Solid
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분자량 403.34
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화학식 C19H19BrN2OS
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Color Off-white to light yellow
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SMILES
CCC1=NC=CC(C2=NC(C)=C(S2)COCC3=CC=C(C=C3)Br)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 10 mg/mL (24.79 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.48 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.48 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4793 mL | 12.3965 mL | 24.7930 mL | 61.9824 mL |
| 5 mM | 0.4959 mL | 2.4793 mL | 4.9586 mL | 12.3965 mL | |
| 10 mM | 0.2479 mL | 1.2396 mL | 2.4793 mL | 6.1982 mL | |
| 15 mM | 0.1653 mL | 0.8264 mL | 1.6529 mL | 4.1322 mL | |
| 20 mM | 0.1240 mL | 0.6198 mL | 1.2396 mL | 3.0991 mL |
WB403 Related Classifications
HY-120565 Related Classifications
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