Potent and selective GPR39 agonist
Potent and selective GPR39 agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). Selective over a panel of kinases (IC50s > 10 μM) and displays minimal binding affinity for ghrelin and neurotensin-1 receptors (IC50s > 30 μM). Increases GLP-1 levels in vitro and in vivo. Reduces TNF-α-induced oxidative stress, mitochondrial dysfunction, cytokine expression and secretion of MMPs in fibroblast-like synoviocytes (FLS). Orally bioavailable.
TC-G 1008 is a potent and selective GPR39 agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). Selective over a panel of kinases (IC50s > 10 μM) and displays minimal binding affinity for ghrelin and neurotensin-1 receptors (IC50s > 30 μM). Increases GLP-1 levels
in vitro
in vivo
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151374 |
| Réf. fabricant | 18730528 |
| Nom chimique ou matériau | TC-G 1008 |
| CAS | 1621175-65-2 |
| Synonyme | N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonate |
| Quantité | 50 mg |
| Solubilité | Soluble to 20mM in DMSO |
| Formule moléculaire | C<sub>1</sub><sub>8</sub>H<sub>1</sub><sub>9</sub>ClN<sub>6</sub>O<sub>2</sub>S |
| Poids de la formule | 418.9 |
| Forme physique | Solid |
| Type de produit | Bioactive Small Molecule |
| Pureté | >98% |
