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PF-00446687 Sale

目录号 : GC32420

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 ± 1nM。

PF-00446687 Chemical Structure

Cas No.:862281-92-3

规格 价格 库存 购买数量
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Sample solution is provided at 25 µL, 10mM.

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产品描述

PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM[1]. Pf-446687 is brain penetrant[2].

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].

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].

[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.

Chemical Properties

Cas No. 862281-92-3 SDF
Canonical SMILES O=C([C@H]1[C@H](C2=C(C=C(F)C=C2)F)CN(C(C)(C)C)C1)N3C[C@H]([C@](O)(C4=CC=CC=C4)[C@@H](C)C3)C
分子式 C28H36F2N2O2 分子量 470.59
溶解度 DMSO: 62.5 mg/mL (132.81 mM) 储存条件 Store at -20°C
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1 mM 2.125 mL 10.625 mL 21.2499 mL
5 mM 0.425 mL 2.125 mL 4.25 mL
10 mM 0.2125 mL 1.0625 mL 2.125 mL
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