TC-G-1008
Based on 5 publication(s) in Google Scholar
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.36%
- CAS. Nr.: 1621175-65-2
- Formel: C18H19ClN6O2S
- Molecular Weight:418.90
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TC-G-1008
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Biologische Aktivität
IC50: 0.4 nM (GPR39), 0.8 nM (GPR39)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.06 nM
Compound: 3
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Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assay
Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assay
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[PMID: 25313322] |
| HEK293 | EC50 |
0.4 nM
Compound: 3
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Agonist activity at rat GPR39 expressed in HEK293 cells by IP1 assay
Agonist activity at rat GPR39 expressed in HEK293 cells by IP1 assay
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[PMID: 25313322] |
| HEK293 | EC50 |
0.8 nM
Compound: 3
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Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assay
Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assay
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[PMID: 25313322] |
| INS-1E | EC50 |
0.02 μM
Compound: 3
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Protection against cytokine-induced cell death in rat INS-1E cells assessed as caspase 3/7 activity
Protection against cytokine-induced cell death in rat INS-1E cells assessed as caspase 3/7 activity
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[PMID: 25313322] |
TC-G-1008 shows selectivity over a panel of kinases (IC50s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM)[1]. In HEK293-GPR39 cells, GPR39-C3, which is a positive allosteric modulator, activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1621175-65-2
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Appearance Solid
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Molecular Weight 418.90
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Formel C18H19ClN6O2S
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Color White to off-white
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SMILES
CS(=O)(NC1=CC=C(CNC2=NC(NC)=NC(C3=NC=CC=C3)=C2)C(Cl)=C1)=O
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Synonyms
GPR39-C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Neural Regen Res
2024 Mar;19(3):687-696. PMID: 37721302 -
Biochem Pharmacol
Dysfunction in the SOCE/EDH-mediated vasorelaxation of mesenteric arteries impairs intestinal barrier integrity in irritable bowel syndrome. [Abstract]2026 Jun 18;251(Pt 2):118179. PMID: 42315077 -
Transl Stroke Res
GPR39 Agonist TC-G 1008 Promoted Mitochondrial Biogenesis and Improved Antioxidative Capability via CREB/PGC-1α Pathway Following Intracerebral Hemorrhage in Mice. [Abstract]2025 Jun;16(3):625-644. PMID: 38485864 -
Clin Exp Pharmacol Physiol
GPR39 Activation Attenuates AngII-Induced Abdominal Aortic Aneurysm by Suppressing ETS-1 Mediated VEGF-A/VEGFR2 Signalling. [Abstract]2025 Aug;52(8):e70053. PMID: 40583196 -
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (238.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.97 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.97 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 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.
Protokoll
HEK293-GPR39 cells are plated and cultured in poly-d-lysine-coated, white, 384-well plates (4000 cells/well) in the growth medium overnight at 37°C in the presence of 5% CO2. For pretreatment of the cells with GPR39 ligands (TC-G-1008) or vehicle control (DMSO), the culture medium is removed and the cells are stimulated with GPR39 ligands in assay buffer for the indicated time at 37°C. Then, the compound solution is removed and washed twice with PBS containing 0.1% BSA. For measurement of intracellular cAMP, the cells are stimulated with drugs in stimulation buffer for 30 min at 37°C. The intracellular cAMP level is determined by using HTRF cAMP dynamic 2 kit[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Peukert S, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8. [Content Brief]
[2]. Shimizu Y, et al. Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation. Biochem Pharmacol. 2017 Sep 15;140:105-114. [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 | 2.3872 mL | 11.9360 mL | 23.8720 mL | 59.6801 mL |
| 5 mM | 0.4774 mL | 2.3872 mL | 4.7744 mL | 11.9360 mL | |
| 10 mM | 0.2387 mL | 1.1936 mL | 2.3872 mL | 5.9680 mL | |
| 15 mM | 0.1591 mL | 0.7957 mL | 1.5915 mL | 3.9787 mL | |
| 20 mM | 0.1194 mL | 0.5968 mL | 1.1936 mL | 2.9840 mL | |
| 25 mM | 0.0955 mL | 0.4774 mL | 0.9549 mL | 2.3872 mL | |
| 30 mM | 0.0796 mL | 0.3979 mL | 0.7957 mL | 1.9893 mL | |
| 40 mM | 0.0597 mL | 0.2984 mL | 0.5968 mL | 1.4920 mL | |
| 50 mM | 0.0477 mL | 0.2387 mL | 0.4774 mL | 1.1936 mL | |
| 60 mM | 0.0398 mL | 0.1989 mL | 0.3979 mL | 0.9947 mL | |
| 80 mM | 0.0298 mL | 0.1492 mL | 0.2984 mL | 0.7460 mL | |
| 100 mM | 0.0239 mL | 0.1194 mL | 0.2387 mL | 0.5968 mL |
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