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BI-135585 is an orally active, selective and potent inhibitor of human 11β-hydroxysteroid dehydrogenase-1 (HSD1) for the study of type 2 diabetes.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $290 | In Stock | In Stock | |
| 5 mg | $650 | In Stock | In Stock | |
| 10 mg | $980 | In Stock | In Stock | |
| 25 mg | $1,670 | In Stock | In Stock | |
| 50 mg | $2,180 | - | In Stock |
| Description | BI-135585 is an orally active, selective and potent inhibitor of human 11β-hydroxysteroid dehydrogenase-1 (HSD1) for the study of type 2 diabetes. |
| Targets&IC50 | the enzyme activity in abdominal subcutaneous adipose tissue (cynomolgus monkey):100 nM, conversion of corticosterone to cortisol:11 nM, 11β-HSD1:1 nM, the enzyme activity in perirenal adipose tissue (cynomolgus monkey):10 nM |
| In vitro | BI-135585 interacts with the substrate binding pocket of the 11β-HSD1 active site. In human preadipocytes, its inhibition of 11β-HSD1 activity was evaluated and found to have an average IC50 of 1 nM. In isolated human adipose tissue, BI-135585 blocked the conversion of corticosterone to cortisol at an average IC50 of 11 nM. [1] A study of abdominal subcutaneous and perirenal adipose tissue from a male cynomolgus monkey showed that BI-135585 (20 hours of action) exhibited dose-dependent inhibition of the enzyme activity in perirenal adipose tissue with an IC50 of approximately 10 nM, while in abdominal subcutaneous adipose tissue the IC50 was approximately 100 nM.[1] |
| In vivo | BI-135585 (compound 11j; 1-3 mg/kg; orally) inhibited the enzyme activity in perirenal adipose tissue of cynomolgus monkeys by 67% and 90%, respectively. [2] |
| Synonyms | BI135585, BI 135585 |
| Molecular Weight | 460.57 |
| Formula | C28H32N2O4 |
| Cas No. | 1114561-85-1 |
| Smiles | C(C(C)(C)O)[C@]1(OC(=O)N([C@@H](C)C2=CC=C(C=C2)C3=CC(=O)N(C)C=C3)CC1)C4=CC=CC=C4 |
| Relative Density. | no data available |
| Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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