TC-G 1005
Based on 1 Customer Validation
TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
For research use only. We do not sell to patients.
- Purity: 99.34%
- CAS No.: 1415407-60-1
- Formula: C25H25N3O2
- Molecular Weight:399.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 0.72 nM (hTGR5); 6.2 nM (mTGR5)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.72 nM
Compound: 23g
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Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay
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[PMID: 23148522] |
| HEK293 | EC50 |
6.2 nM
Compound: 23g
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Agonist activity at mouse TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay
Agonist activity at mouse TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay
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[PMID: 23148522] |
TC-G 1005 activates human and mouse TGR5 with EC50s of 0.72 nM and 6.2 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? TC-G 1005 (50 mg/kg; a single p.o.) causes a 49% reduction in blood glucose AUC0-120 min in ICR mice[1].
? TC-G 1005 (50 mg/kg; a single p.o.) signi?cantly reduces blood glucose at 4, 6, 10, and 24 h in db/db mice[1].
? TC-G 1005 (5 mg/kg; p.o.) exhibits rather low plasma exposure, with a Cmax of 56 ng/mL and a t1/2 of 1.5 in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice[1]
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Dosage:25, 50, 100 mg/kg
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Administration:A single p.o.
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Result:Increased the plasma active GLP-1 levels by 31, 96, and 282% at doses of 25, 50, and 100 mg/kg, respectively.
Chemical Information
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CAS No. 1415407-60-1
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Appearance Solid
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Molecular Weight 399.48
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Formula C25H25N3O2
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Color Off-white to yellow
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SMILES
O=C(C1=CN=CC=C1OC2=C(C=CC(C)=C2)C)N3C4=CC=CC=C4N(C5CC5)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 33.33 mg/mL (83.43 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Purity & Documentation
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Data Sheet (275 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
[1]. Duan H, et, al. Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J Med Chem. 2012 Dec 13;55(23):10475-89. [Content Brief]
[2]. Urso A, et, al. Bile acids inhibit cholinergic constriction in proximal and peripheral airways from humans and rodents. Am J Physiol Lung Cell Mol Physiol. 2020 Feb 1;318(2):L264-L275. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5033 mL | 12.5163 mL | 25.0325 mL | 62.5814 mL |
| 5 mM | 0.5007 mL | 2.5033 mL | 5.0065 mL | 12.5163 mL | |
| 10 mM | 0.2503 mL | 1.2516 mL | 2.5033 mL | 6.2581 mL | |
| 15 mM | 0.1669 mL | 0.8344 mL | 1.6688 mL | 4.1721 mL | |
| 20 mM | 0.1252 mL | 0.6258 mL | 1.2516 mL | 3.1291 mL | |
| 25 mM | 0.1001 mL | 0.5007 mL | 1.0013 mL | 2.5033 mL | |
| 30 mM | 0.0834 mL | 0.4172 mL | 0.8344 mL | 2.0860 mL | |
| 40 mM | 0.0626 mL | 0.3129 mL | 0.6258 mL | 1.5645 mL | |
| 50 mM | 0.0501 mL | 0.2503 mL | 0.5007 mL | 1.2516 mL | |
| 60 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.0430 mL | |
| 80 mM | 0.0313 mL | 0.1565 mL | 0.3129 mL | 0.7823 mL |
TC-G 1005 Related Classifications
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