| Name | TC-G-1008 |
| Description | TC-G-1008 (GPR39-C3) is a zinc receptor agonist with EC50 values of 0.4 nM for rat GPR39 and 0.8 nM for human GPR39. |
| Kinase Assay | 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 (TCG-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] . |
| Animal Research | Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1] . |
| In vitro | TC-G-1008 demonstrates selectivity over a panel of kinases (IC50s>10 μM) and lacks significant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM)[1]. GPR39-C3 acts as a positive allosteric modulator in HEK293-GPR39 cells, activating cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment, and induces dose- and time-dependent loss of response in cAMP production upon second challenge[2]. |
| In vivo | Rat and mouse plasma protein binding for TC-G-1008 is 99.3% and 99.1%, respectively. TC-G-1008 is the first potent GPR39 agonist (EC50s ≤ 1 nM for human and rat receptor) that is orally bioavailable in mice and significantly induces acute GLP-1 levels. Following single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves maximal exposures of 1.4, 6.1, and 25.3 μM, respectively, between 1 and 1.5 hours[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (131.3 mM)
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| Keywords | inhibit | GHSR | TC-G 1008 | Inhibitor | TC-G-1008 | TC-G1008 | Growth hormone secretagogue receptor | TC G 1008 | TCG1008 |
| Inhibitors Related | Ibutamoren Mesylate | Capromorelin Tartrate | AnaMorelin hydrochloride | YIL 781 | Anamorelin | CJC-1295 acetate(863288-34-0 free base) | hGPR91 antagonist 1 | L-692429 | NF-56-EJ40 hydrochloride | TM-N1324 | Obestatin (rat) acetate | Cortistatin-8 acetate |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
