MK5046

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510344

CAS#: 1022152-70-0

Description: MK5046 is a novel bombesin receptor subtype-3 agonist. MK5046 effectively reduced body weight in rats and caused modest increases in body temperature, heart rate, and blood pressure. 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 may be useful for treatment of obesity.


Chemical Structure

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MK5046
CAS# 1022152-70-0

Theoretical Analysis

MedKoo Cat#: 510344
Name: MK5046
CAS#: 1022152-70-0
Chemical Formula: C20H18F6N4O
Exact Mass: 444.13848
Molecular Weight: 444.37
Elemental Analysis: C, 54.06; H, 4.08; F, 25.65; N, 12.61; O, 3.60

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Synonym: MK5046; MK-5046; MK 5046.

IUPAC/Chemical Name: (S)-2-(4-(1H-pyrazol-1-yl)phenyl)-1,1,1-trifluoro-3-(4-((1-(trifluoromethyl)cyclopropyl)methyl)-1H-imidazol-2-yl)propan-2-ol

InChi Key: UJINBEQCDMOAHM-SFHVURJKSA-N

InChi Code: InChI=1S/C20H18F6N4O/c21-19(22,23)17(6-7-17)10-14-12-27-16(29-14)11-18(31,20(24,25)26)13-2-4-15(5-3-13)30-9-1-8-28-30/h1-5,8-9,12,31H,6-7,10-11H2,(H,27,29)/t18-/m0/s1

SMILES Code: O[C@@](CC1=NC(CC2(C(F)(F)F)CC2)=CN1)(C3=CC=C(N4N=CC=C4)C=C3)C(F)(F)F

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 444.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Lateef DM, Abreu-Vieira G, Xiao C, Reitman ML. Regulation of body temperature and brown adipose tissue thermogenesis by bombesin receptor subtype-3. Am J Physiol Endocrinol Metab. 2014 Mar;306(6):E681-7. doi: 10.1152/ajpendo.00615.2013. Epub 2014 Jan 22. PubMed PMID: 24452453; PubMed Central PMCID: PMC3948979.

2: Moreno P, Mantey SA, Nuche-Berenguer B, Reitman ML, González N, Coy DH, Jensen RT. Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors. J Pharmacol Exp Ther. 2013 Oct;347(1):100-16. doi: 10.1124/jpet.113.206896. Epub 2013 Jul 26. PubMed PMID: 23892571; PubMed Central PMCID: PMC3781414.

3: Reitman ML, Dishy V, Moreau A, Denney WS, Liu C, Kraft WK, Mejia AV, Matson MA, Stoch SA, Wagner JA, Lai E. Pharmacokinetics and pharmacodynamics of MK-5046, a bombesin receptor subtype-3 (BRS-3) agonist, in healthy patients. J Clin Pharmacol. 2012 Sep;52(9):1306-16. doi: 10.1177/0091270011419854. Epub 2011 Dec 12. PubMed PMID: 22162541.

4: 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. Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther. 2011 Feb;336(2):356-64. doi: 10.1124/jpet.110.174763. Epub 2010 Oct 29. PubMed PMID: 21036912.

 



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