Description
INCB13739 is an orally active, potent, selective and tissue-specific 11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC 50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity researchIn VitroINCB13739 is >1000-fold selective towards 11β-HSD2, mineralocorticoid receptor (MR), and glucocorticoid receptor (GR). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoINCB13739 (Orally) is effectively distributed in the adipose tissue and is inhibiting 11β-HSD1 activity > 90% for at least 24 h post-dose. INCB13739 (3 mg/kg, IV; 10 mg/kg, PO; once) displays decent oral bioavailability in both rats and cynomolgus monkeys. Pharmacokinetic Parameters of INCB13739 in rats. IV (3 mg/kg) PO (10 mg/kg) C max (µM) 6.46 ± 2.41 AUC 0-24 (ng/mL∗h) 11.2 ± 3.27 t 1/2 (h) 1.4 ± 0.2 1.2 ± 0.3 CL ((L/h)/kg) 1.0 ± 0.2 Vdss (L/kg) 1.6 ± 0.5 F (%) 51 ± 15 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Rats, cynomolgus monkeys Dosage: 3 mg/kg (IV), 10 mg/kg (PO) Administration: IV and PO, once (Pharmacokinetic Analysis) Result: Displayed decent oral bioavailability in both rats (F%=51 ± 15%) and cynomolgus monkeys (F%=43%).Form:SolidIC50& Target:IC50: 3.2 nM (11β-HSD1 enzymatic), 1.1 nM (11β-HSD1 PBMC)