| Identification | Back Directory | [Name]
Methanone, [(3S,4R)-4-(2,4-difluorophenyl)-1-(1,1-diMethylethyl)-3-pyrrolidinyl][(3R,5S)-4-hydroxy-3,5-diMethyl-4-phenyl-1-piperidinyl]- | [CAS]
862281-92-3 | [Synonyms]
PF00446687,PF 00446687
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]-[(3S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl]methanone
Methanone, [(3S,4R)-4-(2,4-difluorophenyl)-1-(1,1-diMethylethyl)-3-pyrrolidinyl][(3R,5S)-4-hydroxy-3,5-diMethyl-4-phenyl-1-piperidinyl]- | [Molecular Formula]
C28H36F2N2O2 | [MDL Number]
MFCD18251471 | [MOL File]
862281-92-3.mol | [Molecular Weight]
470.59 |
| Chemical Properties | Back Directory | [Boiling point ]
571.9±50.0 °C(Predicted) | [density ]
1.167±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 62.5 mg/mL (132.81 mM) | [form ]
Solid | [pka]
13.86±0.60(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12?±?1 nM[1]. Pf-446687 is brain penetrant[2]. | [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]. | [IC 50]
MC4R | [storage]
Store at -20°C | [References]
[1] Lansdell MI, et al. Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans. J Med Chem. 2010 Apr 22;53(8):3183-97. DOI:10.1021/jm9017866
[2] Modi ME, et al. Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015 Jul;40(8):1856-65. DOI:10.1038/npp.2015.35 |
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| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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