INCB13739

Name: INCB13739
Brand: TargetMol
SKU: T60203
Price: 113 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T60203Cas号 869974-19-6

INCB13739是一种具有口服活性、高效、选择性及组织特异性的11β-HSD1抑制剂，对11β-HSD1酶的IC50为3.2 nM，对11β-HSD1 PBMC的IC50为1.1 nM。适用于2型糖尿病(T2DM)和肥胖的研究。

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产品介绍

生物活性

产品描述	INCB13739 is an orally active, potent, selective, and tissue-specific inhibitor of 11β-HSD1 (11β-hydroxysteroid dehydrogenase 1), demonstrating IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC). It is utilized in research for type 2 diabetes mellitus (T2DM) and obesity [1].
体外活性	INCB13739 is over 1000-fold selective for 11β-HSD2, mineralocorticoid receptor (MR), and glucocorticoid receptor (GR) [1].
体内活性	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) shows 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) 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 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%).