| Cat. No. |
Product Name |
CAS No. |
Information |
| GY10208 |
BMS-823778 free base
|
1140897-32-0 |
BMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2; exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg), also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg).
|
| GY06903 |
INCB13739
|
872506-67-7 |
INCB13739 (INCB-13739) is a potent, selective, oral 11βHSD1 inhibitor (IC50=1.1 nM) with high seelctivity over other dehydrogenases, glucocorticoid and mineralocorticoid receptors. |
| GY06902 |
HSD-016
|
946396-92-5 |
HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively; significantly inhibits the 11β-HSD1 activity in mice 3T3-L1 adipocytes with IC50 of 362 nM; HSD-016 (HSD016) has entered phase I clinical trials for the treatment of diabetes. |
| GY06901 |
INU-101
|
1513828-41-5 |
INU-101 (INU101) is a highly potent, selective, orally acitve 11β-HSD1 inhibitor with IC50 of 26.2 nM, 37 nM and 0.6 nM for mice, rats, and human 11β-HSD1, respectively; displays good selectivity for human 11β-HSD1 over 11β-HSD2 (IC50>10 uM); significantly inhibits the 11β-HSD1 activity in mice 3T3-L1 adipocytes (IC50=9.1 nM), enhances insulin sensitivity and lowers the fasting blood glucose level in KKAy mice, ob/ob mice and ZDF rats after oral administration, decreases the body weight and ameliorates an improved lipid profile in the diabetic mouse model. |
| GY06798 |
ASP3662
|
1204178-50-6 |
ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM; demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.); inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord; ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats. |
| GY06678 |
AZD 4017
|
1024033-43-9 |
AZD4017 is a potent, selective, and orally bioavailable human 11β-HSD1 with IC50 of 7 nM, shows no significant activity against 11β-HSD1 and 17β-HSD1, 17β-HSD3 (IC50>30 uM); AZD4017 is inactive (<25% inhibition at 10 μM) against Cytochrome P450 enzymes (CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4), and lower potency against the mouse, rat and dog 11β-HSD1 (IC50=750-4000 nM); demonstrates the dose dependent inhibition of 11β-HSD1 in vivo. |
| GY04220 |
BVT 2733
|
376640-41-4 |
BVT 2733 is a non-steroidal, isoform-selective inhibitor of mouse 11β-HSD1 with Ki of 1 uM; displays >20-fold selectivity over 11β-HSD2; lowers hepatic PEPCK and glucose-6-phosphatase mRNA, blood glucose and serum insulin concentrations in a hyperglycaemic and hyperinsulinaemic mouse model. |
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