Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TC-G-1008 (GPR39-C3) is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
説明 | TC-G-1008 (GPR39-C3) is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). |
ターゲット&IC50 | rat GPR39 :0.4 nM, GPR139 (human):0.8 nM |
In vitro | 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]. GPR39-C3 is a positive allosteric modulator in HEK293-GPR39 cells which 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]. |
In vivo | Rat and mouse plasma protein binding for TC-G-1008 is measured as 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 robustly induced acute GLP-1 levels. Upon 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, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively[1]. |
キナーゼ試験 | 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] . |
動物実験 | Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1] . |
別名 | GPR39-C3 |
分子量 | 418.9 |
分子式 | C18H19ClN6O2S |
CAS No. | 1621175-65-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (131.3 mM)
You can also refer to dose conversion for different animals. 詳細
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TC-G-1008 1621175-65-2 GPCR/G Protein GHSR inhibit GPR39-C3 TC-G 1008 Inhibitor TC-G1008 Growth hormone secretagogue receptor TC G 1008 TCG1008 inhibitor