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Cat. No. Product Name CAS No. Information
PC-45743

Setmelanotide

920014-72-8

Setmelanotide (RM-493, BIM-22493, IRC-022493) is a peptide, non-selective melanocortin receptor agonist with binding Ki of 3.9/10/2.1 for hMC1R/hMC3R/hMC4R, respectively; exhibits weak activity at MC5R (EC50>1 uM) and inactive at the mouse MC2R (EC50>10 uM); acutely improves glucose homeostasis, causes weight loss and improves hyperinsulinemia and fatty liver in diet induced obese mice.

Obesity

Phase 3 Clinical

PC-36115

RO 27-3225

RO 27-3225 (RO27-3225, RO 273225) is a potent, selective melanocortin melanocortin receptor MC4R agonist with EC50 of 1 nM, >30-fold selectivity over MC3R; shows some activity at the MC1 receptor (EC50=8 nM), reverses hemorrhagic shock, reduces multiple organ damage, and improves survival.

Obesity

Discontinued

PC-35972

MLN-4760

305335-31-3 MLN-4760 (MLN4760) is a potent, selective inhibitor of angiotensin-converting enzyme (ACE)-related carboxypeptidase ACE2 with IC50 of 0.44 nM (hACE2); displays >5,000-fold selectivity over related enzymes including human testicular ACE (IC50>100 uM) and bovine carboxypeptidase A (IC50=27 uM); exacerbated the Ang II-dependent formation of ROS and abolished the generation of Ang-(1-7) from Ang II; exacerbates cardiac hypertrophy and fibrosis in Ren-2 hypertensive rats.

Obesity

Phase 1 Discontinued

PC-62952

JTT-553 benzosulfonate

JTT-553 is a novel potent, selective DGAT-1 inhibitor with IC50 of 2.38 nM, shows no inhibitory activity for human DGAT2 and ACA T1 (IC50>10 uM); suppresses plasma TG and chylomicron TG levels after olive oil loading in Sprague-Dawley (SD) rats; also reduces daily food intake and body weight gain in diet-induced obesity rats.

Obesity

Phase 1 Discontinued

PC-62951

JTT-553

701232-94-2 JTT-553 is a novel potent, selective DGAT-1 inhibitor with IC50 of 2.38 nM, shows no inhibitory activity for human DGAT2 and ACA T1 (IC50>10 uM); suppresses plasma TG and chylomicron TG levels after olive oil loading in Sprague-Dawley (SD) rats; also reduces daily food intake and body weight gain in diet-induced obesity rats.

Obesity

Phase 1 Discontinued

PC-62766

AZD 8329

1048668-70-7 AZD8329 is a potent, selective 11β-HSD1 inhibitor with IC50 of 9 nM, displays excellent selectivity versus relatedd 11β-HSD2, 17β-HSD1 and 17β-HSD3 (IC50>30 uM); shows significantly reduced acyl glucuronidation liability compared with AZD4017.

Obesity

Phase 1 Discontinued

PC-62525

BIBO 3304

191868-14-1 BIBO 3304 is a potent, selective, nonpeptide neuropeptide Y Y1 receptor antagonist with IC50 of 0.38 and 0.72 nM for human and the rat Y1 receptor, respectively; shows low affinity for the human Y2 receptor, human and rat Y4 receptor, human and rat Y5 receptor (IC50>1,000 nM); inhibits the feeding response induced by 1 mg NPY in mice, also completely abolishes PYY-induced inhibition of insulin release in vivo.

Obesity

Discontinued

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