MK-5046
MK-5046 Basic information
- Product Name:
- MK-5046
- Synonyms:
-
- MK-5046
- MK5046 peak 2
- (2S)-1,1,1-TRIFLUORO-2-(4-PYRAZOL-1-YLPHENYL)-3-[5-[[1-(TRIFLUOROMETHYL)CYCLOPROPYL]METHYL]-1H-IMIDAZOL-2-YL]PROPAN-2-OL
- (alphaS)-alpha-[4-(1H-Pyrazol-1-yl)phenyl]-alpha-(trifluoromethyl)-5-[[1-(trifluoromethyl)cyclopropyl]methyl]-1H-imidazole-2-ethanol
- CS-2034
- (2S)-1,1,1-Trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]-3-(4-{[1-(trif luoromethyl)cyclopropyl]methyl}-1H-imidazol-2-yl)-2-propanol
- 1H-Imidazole-2-ethanol, α-[4-(1H-pyrazol-1-yl)phenyl]-α-(trifluoromethyl)-5-[[1-(trifluoromethyl)cyclopropyl]methyl]-, (αS)-
- CAS:
- 1022152-70-0
- MF:
- C20H18F6N4O
- MW:
- 444.38
- Product Categories:
-
- Inhibitors
- Mol File:
- 1022152-70-0.mol
MK-5046 Chemical Properties
- Boiling point:
- 571.6±50.0 °C(Predicted)
- Density
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 11.22±0.15(Predicted)
- color
- White to light yellow
MK-5046 Usage And Synthesis
Uses
MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity[1][2][3].
in vivo
MK-5046 (3, 10 and 30 mg/kg; oral administration for once) inhibits food intake, and increases resting metabolic rate (MR) and body temperature in DIO mice[1]. MK-5046 (5, 25 and 50 mg/kg; s.c. once daily for 14 days) significantly reduces body weight and food intake in DIO mice[1].
| Animal Model: | Male C57BL/6N mice with high-fat diet for the diet-induced obese (DIO) model[1] |
| Dosage: | 3, 10 and 30 mg/kg |
| Administration: | Oral administration; 3, 10 and 30 mg/kg for once |
| Result: | Dose-dependently inhibited food intake at 2 h and overnight in DIO mice. But showed no effect on Brs3 knockout mice. |
References
[1] Guan XM, et al. Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther. 2011 Feb;336(2):356-364. DOI:10.1124/jpet.110.174763
[2] Sebhat IK, et al. Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett. 2010 Oct 18;2(1):43-47. DOI:10.1021/ml100196d
[3] Ramos-Alvarez I, et al. The Nonpeptide Agonist MK-5046 Functions As an Allosteric Agonist for the Bombesin Receptor Subtype-3. J Pharmacol Exp Ther. 2022 Aug;382(2):66-78. DOI:10.1124/jpet.121.001033
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