862281-92-3
862281-92-3 structure
- Name: PF-00446687
- Chemical Name: [(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]-[(3S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl]methanone
- CAS Number: 862281-92-3
- Molecular Formula: C28H36F2N2O2
- Molecular Weight: 470.59400
- Catalog: Research Areas Endocrinology
- Create Date: 2016-06-26 00:26:55
- Modify Date: 2024-01-11 11:13:43
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PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM[1]. Pf-446687 is brain penetrant[2].
| Name | [(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]-[(3S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl]methanone |
|---|---|
| Synonyms | unii-63p236z73i |
| Description | PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM[1]. Pf-446687 is brain penetrant[2]. |
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| Related Catalog | |
| Target |
EC50: 12 ± 1 nM (MC4R)[1] |
| In Vitro | PF-00446687 binds MC4 receptor with a Ki of 27±4 nM. PF-00446687 has a relatively weak activity at the MC1, MC3, and MC5 receptors with EC50s of 1.02±0.30 μM, 1.16±0.35 μM, and 1.98±0.20 μM, respectively. The broad off-target profiles of PF-00446687 are assessed in the CEREP Bioprint wide ligand screening panel, with the most potent binding activities being at the σ receptor (Ki=330 nM), the sodium ion channel (Ki=690 nM), and the muscarinic M2 receptor (Ki=730 nM)[1]. |
| In Vivo | Pf-446687 is highly selective for MC4R and is both brain penetrant and stable in vivo. Peripheral administration of the brain penetrant MC3/4R receptor peptide agonist, Melanotan II (MTII), and the highly selective, small molecule MC4R agonist, Pf-446687, enhances partner preference formation in the prairie vole, but not in the non-monogamous meadow vole[2]. |
| References |
| Molecular Formula | C28H36F2N2O2 |
|---|---|
| Molecular Weight | 470.59400 |
| Exact Mass | 470.27400 |
| PSA | 43.78000 |
| LogP | 4.65670 |