TC-G-1008
TC-G-1008
CAS: 1621175-65-2
Molecular Formula: C18H19ClN6O2S
TC-G-1008 - Names and Identifiers
TC-G-1008 - Physico-chemical Properties
| Molecular Formula | C18H19ClN6O2S |
| Molar Mass | 418.9 |
| Density | 1.462±0.06 g/cm3(Predicted) |
| Boling Point | 662.1±65.0 °C(Predicted) |
| Solubility | DMSO: ≥100 mg/mL |
| pKa | 7.43±0.10(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | TC-G-1008 shows selectivity over a panel of kinases (IC 50 s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC 50 s>30 μM). 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. |
| In vivo study | Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in mice and robustly induces 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. |
TC-G-1008 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.387 ml | 11.936 ml | 23.872 ml |
| 5 mM | 0.477 ml | 2.387 ml | 4.774 ml |
| 10 mM | 0.239 ml | 1.194 ml | 2.387 ml |
| 5 mM | 0.048 ml | 0.239 ml | 0.477 ml |
Last Update：2024-01-02 23:10:35
TC-G-1008 - Reference Information
| biological activity | TC-G-1008(GPR39-C3) is an effective and orally active G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist, with EC50 values of 0.4 nM and 0.8 nM for rat and human receptors respectively. |
| target | TargetValue rGPR39 (Cell-free assessment) 0.4 nM(EC50) hGPR39 (Cell-free assessment) 0.8 nM(EC50) |
| Target | Value |
| rGPR39 (Cell-free assay) | 0.4 nM(EC50) |
| hGPR39 (Cell-free assay) | 0.8 nM(EC50) |
| in vitro study | TC-G-1008 shows selectivity over a panel of kinases (IC 50 s>10 μ m) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC 50 s>30 μ m). 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 pose-and time-dependent loss of response in cAMP production by second challenge of the compound. |
| in vivo study | Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in ice and robustly induces 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. |
Last Update：2024-04-09 21:54:55
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