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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-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

PC-62017

CL 316243

183720-02-7 CL 316243 (BTA 243) is a potent, highly selective, orally active β3-adrenoceptor agonist with EC50 of 3 nM; Displays >10000-fold selective over β1 and β2 receptors; Significantly increases brown adipose tissue thermogenesis and resting metabolic rate in mice, also increases the concentration of insulin receptors and decreases the levels of serum insulin and blood glucose during the glucose overloading test.

Obesity

Discontinued

PC-62016

CL 316243 disodium

138908-40-4 CL 316243 is a potent, highly selective, orally active β3-adrenoceptor agonist with EC50 of 3 nM; Displays >10000-fold selective over β1 and β2 receptors; Significantly increases brown adipose tissue thermogenesis and resting metabolic rate in mice, also increases the concentration of insulin receptors and decreases the levels of serum insulin and blood glucose during the glucose overloading test.

Obesity

Discontinued

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