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PF-00446687

Catalog No. T12415   CAS 862281-92-3

PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).

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PF-00446687 Chemical Structure
PF-00446687, CAS 862281-92-3
Pack Size Availability Price/USD Quantity
5 mg 10-14 weeks $ 297.00
25 mg 10-14 weeks $ 987.00
50 mg 10-14 weeks $ 1,360.00
100 mg 10-14 weeks $ 1,860.00
1 mL * 10 mM (in DMSO) 10-14 weeks $ 365.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).
Targets&IC50 MC4R:12 ± 1 nM (EC50)
In vitro PF-00446687 has a relatively weak activity at the MC1, MC3, and MC5 receptors(EC50s of 1.02±0.30 μM, 1.16±0.35 μM, and 1.98±0.20 μM, respectively).
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].
Molecular Weight 470.59
Formula C28H36F2N2O2
CAS No. 862281-92-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62.5 mg/mL (132.81 mM), Sonication is recommended.

TargetMolReferences and Literature

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. 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.

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Keywords

PF-00446687 862281-92-3 Others PF 00446687 PF00446687 inhibitor inhibit

 

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