1114561-85-1
1114561-85-1 structure
- Name: BI 135585
- Chemical Name: BI-135585
- CAS Number: 1114561-85-1
- Molecular Formula: C28H32N2O4
- Molecular Weight: 460.565
- Catalog: Research Areas Metabolic Disease
- Create Date: 2018-06-13 15:19:57
- Modify Date: 2024-01-09 21:13:33
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BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research[1][2].
| Name | BI-135585 |
|---|---|
| Synonyms |
(6S)-6-(2-Hydroxy-2-methylpropyl)-3-{(1S)-1-[4-(1-methyl-2-oxo-1,2-dihydro-4-pyridinyl)phenyl]ethyl}-6-phenyl-1,3-oxazinan-2-one
BI-135585 DA4HT8614K 2H-1,3-Oxazin-2-one, 3-[(1S)-1-[4-(1,2-dihydro-1-methyl-2-oxo-4-pyridinyl)phenyl]ethyl]tetrahydro-6-(2-hydroxy-2-methylpropyl)-6-phenyl-, (6S)- |
| Description | BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research[1][2]. |
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| Related Catalog | |
| Target |
IC50: 13 nM (11β-HSD1)[1] |
| In Vitro | BI-135585 binds in the substrate binding pocket of the active site of 11β-HSD1. Cellular activity of BI-135585 is examined by determining inhibition of 11β-HSD1 activity in human preadipocytes, the average IC50 is 1 nM[1]. In human adipose tissue ex vivo, BI-135585 inhibits the conversion of cortisone to cortisol with an average IC50 of 11 nM[1]. Abdominal subcutaneous and perirenal adipose tissue was harvested from one, male cynomolgus monkey. BI-135585 (20 hours) reduces enzyme activity in a dose-dependent manner with an IC50 of ~10 nM in perirenal adipose tissue and an IC50 of ~100 nM in abdominal subcutaneous adipose tissue[1]. |
| In Vivo | BI-135585 (compound 11j; 1-3 mg/kg; po) inhibits 67% and 90% of enzyme activity respectively in perirenal adipose tissue in cynomolgus monkey[2]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 703.6±60.0 °C at 760 mmHg |
| Molecular Formula | C28H32N2O4 |
| Molecular Weight | 460.565 |
| Flash Point | 379.3±32.9 °C |
| Exact Mass | 460.236206 |
| LogP | 3.69 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.596 |