MK-5046
Modify Date: 2024-01-30 14:58:46
MK-5046 structure
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Common Name | MK-5046 | ||
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| CAS Number | 1022152-70-0 | Molecular Weight | 444.37400 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C20H18F6N4O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of MK-5046MK-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-3in 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] |
| Name | (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 |
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| Synonym | More Synonyms |
| Description | 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-3in 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] |
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| Related Catalog | |
| References |
| Molecular Formula | C20H18F6N4O |
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| Molecular Weight | 444.37400 |
| Exact Mass | 444.13800 |
| PSA | 66.73000 |
| LogP | 4.47300 |
| Storage condition | 2-8℃ |
| MK-5046 |