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Cat. No. Product Name CAS No. Information
PC-61492

BMS-823778

1140898-87-8

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).

Diabetes

Phase 2 Clinical

PC-60448

BI 135585

1114561-85-1

BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively; exhibits >1,000-fold selectivity over other hydroxysteroid dehydrogenases; inhibits 11β HSD1 activity in adipose tissue, displays desirable pharmacodynamic properties in vivo.

Diabetes

Phase 1 Clinical

PC-60371

UE2343

1346013-80-6

UE2343 (UE-2343, Xanamem) is a potent, orally bioavailable, brain penetrant 11β-HSD1 inhibitor with IC50 of 24 nM in cell-free assays, with no activity for isozyme 11β-HSD2; displays a superior preclinical profile for further development, and shows potential for cognitive impairment in early Alzheimer's disease (AD).

Alzheimer Disease

Phase 2 Clinical

PC-45408

PF-915275

857290-04-1

A specific and potent inhibitor of the human11β-HSD1 with Ki of 2.3 nM and in vitro HEK293 EC50 of 15 nM, with minimal inhibitory activity toward the mouse enzyme (Ki=750 nM); do not significantly inhibit 11βHSD2; dose-dependently inhibits 11betaHSD1-mediated conversion of prednisone to prednisolone (3-mg/kg, 87% inhibition) in cynomolgus monkeys.

PC-45407

BVT-14225

376638-65-2

A selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50 of 52 nM; displays >200-fold selectivity over human and murine 11β-HSD2. reduces glucose levels in diabetic KKA(y) mice.

Diabetes

Preclinical

PC-45406

BVT-2733

376640-41-4

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.

Diabetes

Preclinical

PC-35575

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.

Diabetes

Phase 2 Clinical

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