869974-19-6
869974-19-6 structure
- Name: INCB13739
- Chemical Name: INCB13739
- CAS Number: 869974-19-6
- Molecular Formula: C28H25N3O4
- Molecular Weight: 467.52
- Catalog: Signaling Pathways GPCR/G Protein Glucocorticoid Receptor
- Create Date: 2022-08-31 14:04:21
- Modify Date: 2025-09-11 11:11:10
-
INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 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 research[1].
| Name | INCB13739 |
|---|
| Description | INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 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 research[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 3.2 nM (11β-HSD1 enzymatic), 1.1 nM (11β-HSD1 PBMC)[1] |
| In Vitro | INCB13739 is >1000-fold selective towards 11β-HSD2, mineralocorticoid receptor (MR), and glucocorticoid receptor (GR)[1]. |
| In Vivo | INCB13739 (Orally) is effectively distributed in the adipose tissue and is inhibiting 11β-HSD1 activity > 90% for at least 24 h post-dose[1]. INCB13739 (3 mg/kg, IV; 10 mg/kg, PO; once) displays decent oral bioavailability in both rats and cynomolgus monkeys[1]. Pharmacokinetic Parameters of INCB13739 in rats[1]. IV (3 mg/kg) PO (10 mg/kg) Cmax (µM) 6.46 ± 2.41 AUC0-24 (ng/mL∗h) 11.2 ± 3.27 t1/2 (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 Animal Model: Rats, cynomolgus monkeys[1] 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%). |
| References |
| Molecular Formula | C28H25N3O4 |
|---|---|
| Molecular Weight | 467.52 |