INCB13739

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INCB13739

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

869974-19-6

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

INCB13739 是一种口服有效的、选择性的和组织特异性11β-HSD1(11β- 羟类固醇脱氢酶 1) 抑制剂，IC₅₀值分别为 3.2 nM (11β-HSD1 酶)和 1.1 nM (11β-HSD1 PBMC)。INCB13739 可用于 2 型糖尿病 (T2DM) 和肥胖研究。

生物活性

INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1(11β-hydroxysteroid dehydrogenase 1) inhibitor, withIC₅₀values 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].

IC₅₀& Target

IC50: 3.2 nM (11β-HSD1 enzymatic), 1.1 nM (11β-HSD1 PBMC)^[1]

体外研究
(In Vitro)

INCB13739 is >1000-fold selective towards 11β-HSD2, mineralocorticoid receptor (MR), and glucocorticoid receptor (GR)^[1].

体内研究
(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)
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%).

Clinical Trial

分子量

467.52

Formula

C₂₈H₂₅N₃O₄

CAS 号

869974-19-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.