For research use only. Not for therapeutic Use.
MK-5046 (Cat.No:I000157) is a small-molecule inhibitor of the neurokinin 1 receptor (NK1R). It works by blocking the binding of substance P to NK1R, which is involved in various physiological processes including pain transmission and inflammation. MK-5046 has shown potential as a therapeutic agent for the treatment of chronic pain disorders.
| Catalog Number | I000157 |
| CAS Number | 1022152-70-0 |
| Molecular Formula | C20H18F6N4O |
| Purity | ≥95% |
| Target | Bombesin Receptor |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| IC50 | 1.6 nM (Ki, for mouse), 25 nM (Ki, for human) [1] |
| Reference | </br>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</br>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</br>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</br>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 |
