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

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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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].

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].

Storage

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

References
Molecular Weight

470.59

Formula

C₂₈H₃₆F₂N₂O₂

CAS No.

862281-92-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PF-00446687
Cat. No.:
HY-10622
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PF-00446687

Cat. No.: HY-10622