CAS No. : 1022152-70-0

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For research use only. Not Intended for Therapeutic Use!
Cat No:I000157
Molecular Formula:C20H18F6N4O
Molecular Weight:444.37
IC50:1.6 nM (Ki, for mouse), 25 nM (Ki, for human) [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000157
Cas No:1022152-70-0

MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).
IC50 value: 1.6 nM (Ki, for mouse), 25 nM (Ki, for human) [1]
Target: BRS-3
in vitro: MK-5046 is a novel BRS-3 agonist, with improved BRS-3 potency, specificity, and pharmacokinetic properties that allows in-depth investigation of BRS3 agonism in preclinical species and is also potentially suitable for use in humans. MK-5046 exhibits no appreciable binding activity at the neuromedin B and gastrin-releasing peptide receptors, as well as many other receptors, ion channels, and enzymes. In a cell-based Ca2+ mobilization functional assay, MK-5046 activates human BRS-3 with similar agonist efficacy as the peptide BRS-3 agonist.[1] MK-5046 is a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity.[2]
in vivo: MK-5046 is the first BRS-3 agonist with properties suitable for use in larger mammals. In dogs, MK-5046 treatment produced statistically significant and persistent weight loss, which was initially accompanied by increases in body temperature and heart rate that abated with continued dosing. MK-5046 also effectively reduced body weight in rats and caused modest increases in body temperature, heart rate, and blood pressure. MK-5046 in rodents and dogs and further support BRS-3 agonism as a new approach to the treatment of obesity.[1]

1:Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors. Moreno P, Mantey SA, Nuche-Berenguer B, Reitman ML, González N, Coy DH, Jensen RT.J Pharmacol Exp Ther. 2013 Oct;347(1):100-16. doi: 10.1124/jpet.113.206896. Epub 2013 Jul 26. PMID: 23892571 Free PMC Article
2:Pharmacokinetics and pharmacodynamics of MK-5046, a bombesin receptor subtype-3 (BRS-3) agonist, in healthy patients. Reitman ML, Dishy V, Moreau A, Denney WS, Liu C, Kraft WK, Mejia AV, Matson MA, Stoch SA, Wagner JA, Lai E.J Clin Pharmacol. 2012 Sep;52(9):1306-16. doi: 10.1177/0091270011419854. Epub 2011 Dec 12. PMID: 22162541 Free PMC Article
3:Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. Sebhat IK, Franklin C, Lo MM, Chen D, Jewell JP, Miller R, Pang J, Palyha O, Kan Y, Kelly TM, Guan XM, Marsh DJ, Kosinski JA, Metzger JM, Lyons K, Dragovic J, Guzzo PR, Henderson AJ, Reitman ML, Nargund RP, Wyvratt MJ, Lin LS.ACS Med Chem Lett. 2010 Oct 18;2(1):43-7. doi: 10.1021/ml100196d. eCollection 2011 Jan 13. PMID: 24900253 Free PMC Article
4:Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. Guan XM, Metzger JM, Yang L, Raustad KA, Wang SP, Spann SK, Kosinski JA, Yu H, Shearman LP, Faidley TD, Palyha O, Kan Y, Kelly TM, Sebhat I, Lin LS, Dragovic J, Lyons KA, Craw S, Nargund RP, Marsh DJ, Strack AM, Reitman ML.J Pharmacol Exp Ther. 2011 Feb;336(2):356-64. doi: 10.1124/jpet.110.174763. Epub 2010 Oct 29. PMID: 21036912 Free Article
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