| Identification | Back Directory | [Name]
MK-5046 | [CAS]
1022152-70-0 | [Synonyms]
MK-5046
CS-2034
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
1H-Imidazole-2-ethanol, α-[4-(1H-pyrazol-1-yl)phenyl]-α-(trifluoromethyl)-5-[[1-(trifluoromethyl)cyclopropyl]methyl]-, (αS)-
(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
(alphaS)-alpha-[4-(1H-Pyrazol-1-yl)phenyl]-alpha-(trifluoromethyl)-5-[[1-(trifluoromethyl)cyclopropyl]methyl]-1H-imidazole-2-ethanol | [Molecular Formula]
C20H18F6N4O | [MDL Number]
MFCD18782708 | [MOL File]
1022152-70-0.mol | [Molecular Weight]
444.38 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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.
|
| [storage]
Store at -20°C | [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 |
|
| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Tel: |
020-13556033878 2965585218 13556033878 |
| Website: |
http://m.is0513.com/ShowSupplierProductsList15061/0.htm |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|