产品
编 号：F760945
分子式：C28H25N3O4
分子量：467.52
分子式：C28H25N3O4
分子量：467.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 869974-19-6
产品详情
生物活性：
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.
体内研究：
INCB13739 (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)
Cmax (μM)6.46 ± 2.41
AUC0-24 (ng/mL?h)11.2 ± 3.27
t1/2 (h)1.4 ± 0.21.2 ± 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
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%).
体外研究：
INCB13739 is >1000-fold selective towards 11β-HSD2, mineralocorticoid receptor (MR), and glucocorticoid receptor (GR).
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.
体内研究：
INCB13739 (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)
Cmax (μM)6.46 ± 2.41
AUC0-24 (ng/mL?h)11.2 ± 3.27
t1/2 (h)1.4 ± 0.21.2 ± 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
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%).
体外研究：
INCB13739 is >1000-fold selective towards 11β-HSD2, mineralocorticoid receptor (MR), and glucocorticoid receptor (GR).
产品资料
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