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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $100 | - | 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-HSD1:3.2 nM, 11β-HSD1 (PBMC):1.1 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] |
| Synonyms | 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/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (213.89 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.56 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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