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TC-G 1005
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Catalog No. T8818Cas No. 1415407-60-1
TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.
TC-G 1005
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Purity: 99.78%
Catalog No. T8818Cas No. 1415407-60-1
TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 2 mg | $38 | In Stock | In Stock | |
| 5 mg | $63 | In Stock | In Stock | |
| 10 mg | $97 | In Stock | In Stock | |
| 25 mg | $198 | In Stock | In Stock | |
| 50 mg | $298 | In Stock | In Stock | |
| 100 mg | $445 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $69 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.78%
Appearance:Solid
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Product Introduction
TC-G 1005 AI Summary
TC-G 1005 exhibits multiple bioactivities, including agonist activity at FXR (-3.0% relative efficacy at 10 µM concentration compared to GW4064), mouse TGR5 (EC50 of 6.2 nM), and human TGR5 (EC50 of 0.72 nM). Additionally, it increases GLP1 levels in ICR mouse plasma, with activities ranging from 31.0% to 282.0%, and demonstrates antihyperglycemic activity by reducing glucose AUC by 49.0% in ICR mice. However, it also induces gall bladder toxicity, evidenced by a 231.0% increase in gall bladder volume.
In antiviral assays, TC-G 1005 effectively inhibits SARS-CoV-2-induced cytotoxicity in Caco-2 cells with 97.03% efficacy at 10 µM after 48 hours. It also inhibits SARS-CoV-2 3CL-Pro protease by 21.79% at 20 µM. When tested on VERO-6 cells, it shows negligible inhibition (-0.08%) against SARS-CoV-2-induced cytotoxicity at the same concentration and exposure time.
In addition to its antiviral properties, TC-G 1005 exhibits inhibitory activity in enzymatic assays for human HDAC6, with 10.67% inhibition using a commercial peptide substrate and -16.77% with a custom substrate. Thermal shift assays indicate that the compound alters the thermal stability of various protein domains, suggesting potential interactions.
Moreover, in GPCR beta-arrestin recruitment assays, TC-G 1005 demonstrates inhibitory effects on multiple targets such as ADRA2A, GPR35, AGTR1, S1PR1, FPR2, ADRB2, APLNR, CX3CR1, FFAR4, and C5AR1. It also shows maximal effects on targets like AGTR1, S1PR1, APLNR, ADGRF1, and GPR119, indicating a complex interaction profile with these GPCR targets..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available. |
| Targets&IC50 | TGR5 (human):0.72 nM |
| Molecular Weight | 399.48 |
| Formula | C25H25N3O2 |
| Cas No. | 1415407-60-1 |
| Smiles | Cc1ccc(C)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc23)c1 |
| Relative Density. | 1.253 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (25.03 mM), Sonication is recommended.  | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.5 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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Calculator
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
You can also refer to dose conversion for different animals. More Dose Conversion
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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