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INCB13739 is an orally active, selective, and highly efficient 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. INCB13739 improves hyperglycemia in patients with uncontrolled type 2 diabetes on metformin monotherapy and can be used in hyperlipidemia and hypertriglyceridemia research.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $109 | In Stock | |
5 mg | $238 | In Stock | |
10 mg | $383 | In Stock | |
25 mg | $759 | In Stock | |
50 mg | $1,050 | In Stock | |
100 mg | $1,390 | In Stock | |
200 mg | $1,890 | In Stock | |
1 mL x 10 mM (in DMSO) | $253 | In Stock |
Description | INCB13739 is an orally active, selective, and highly efficient 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. INCB13739 improves hyperglycemia in patients with uncontrolled type 2 diabetes on metformin monotherapy and can be used in hyperlipidemia and hypertriglyceridemia research. |
Targets&IC50 | 11β-HSD1 in PBMC:1.1 nM, 11β-HSD1:3.2 nM |
In vitro | INCB13739 is an orally active, potent, selective, and tissue-specific inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1), with an IC50 of 3.2 nM for 11β-HSD1 enzyme and 1.1 nM for 11β-HSD1 in PBMC. INCB13739 has greater than 1,000-fold selectivity for 11β-HSD2, the salt corticosteroid receptor (MR), and the glucocorticoid receptor (GR). [1] |
In vivo | After oral administration, INCB13739 was efficiently distributed to adipose tissue and inhibited 11β-HSD1 activity by >90% for at least 24 h. INCB13739 (3 mg/kg i.v.; 10 mg/kg orally; single dose) exhibited good oral bioavailability in rats (F%=51%) and cynomolgus monkeys (F%=43%). [1] |
Alias | INCB013739, INCB 13739, INCB 013739 |
Molecular Weight | 467.52 |
Formula | C28H25N3O4 |
Cas No. | 869974-19-6 |
Smiles | C(=O)(C1(CC1)C2=CC=C(C=C2)C=3C=CC(C(NC)=O)=NC3)N4C[C@@]5(CC4)C=6C(C(=O)O5)=CC=CC6 |
Relative Density. | 1.39 g/cm3 (Predicted) |
Storage | keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (213.89 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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