1. GPCR/G Protein
    Neuronal Signaling
  2. Melanocortin Receptor
  3. PF-00446687


Cat. No.: HY-10622
Handling Instructions

PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.

For research use only. We do not sell to patients.

PF-00446687 Chemical Structure

PF-00446687 Chemical Structure

CAS No. : 862281-92-3

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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].

IC50 & 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].

Clinical Trial
Molecular Weight







O=C([[email protected]]1[[email protected]](C2=C(C=C(F)C=C2)F)CN(C(C)(C)C)C1)N3C[[email protected]]([[email protected]](O)(C4=CC=CC=C4)[[email protected]@H](C)C3)C


Room temperature in continental US; may vary elsewhere


Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (132.81 mM; Need ultrasonic)

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1250 mL 10.6250 mL 21.2499 mL
5 mM 0.4250 mL 2.1250 mL 4.2500 mL
10 mM 0.2125 mL 1.0625 mL 2.1250 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
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