851484-58-7

Upstream product

• 851484-56-5 trans-1-tert-butoxycarbonyl-4-(4-chlorophenyl)pyrrolidine-3-carboxylic acid 
• 869478-56-8 (S_S)-2-methyl-propane-2-sulfinic acid [(S)-2-methyl-1-(5-methyl-2-piperazin-1-yl-phenyl)-propyl]-amide 
• 851484-57-6 C₃₅H₅₁ClN₄O₄S 

Relevant academic research and scientific papers

Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor

A series of trans-4-phenylpyrrolidine-3-carboxamides were synthesized and characterized as potent ligands of the human melanocortin-4 receptor. Interestingly, a pair of diastereoisomers 13b displayed potent functional agonist and antagonist activity, resp

Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor

A series of pyrrolidine derivatives were synthesized and characterized as potent agonists of the human melanocortin-4 receptor. For example, 28c had a Ki of 13 nM in binding affinity and EC50 of 6.9 nM in agonist potency with an intr

Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor

A series of trans-4-phenylpyrrolidine-3-carboxamides were synthesized and characterized as potent ligands of the human melanocortin-4 receptor. Interestingly, a pair of diastereoisomers 20f-1 and 20f-2 displayed potent functional agonist and antagonist activity, respectively. Thus, the 3S,4R-compound 20f-1 possessed a Ki of 11 nM and an EC50 of 24 nM, while its 3R,4S-isomer 20f-2 exhibited a Ki of 8.6 and an IC50 of 65 nM. Both compounds were highly selective over other melanocortin receptor subtypes. The MC4R agonist 20f-1 also demonstrated efficacy in diet-induced obese rats.