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PF-00446687

CAS No. : 862281-92-3

MCE 站：PF-00446687

产品活性：PF-00446687 是一种有效的，脑渗透性的，选择性黑皮质素 4 受体 (MC4R) 激动剂，EC50 为 12?±?1 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Melanocortin Receptor

In Vitro: PF-00446687 binds MC4 receptor with a K_i 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 (K_i=330 nM), the sodium ion channel (K_i=690 nM), and the muscarinic M2 receptor (K_i=730 nM).

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.

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