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CAS No. : 862281-92-3
MCE 国际站: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 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).
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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Clinical Compound Library | CNS-Penetrant Compound Library | Drug Repurposing Compound Library | Endocrinology Compound Library | Anti-Obesity Compound Library | Targeted Diversity Library | Chemokine Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | PG106 | Bremelanotide | ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) | ACTH (11-24) | Adrenocorticotropic Hormone (ACTH) (1-39), human(TFA) | MK-0493 | HS024 | Melanotan I acetate | Agouti-related Protein (AGRP) (83-132) Amide (human) | JNJ-10229570 | MCL0020 | MC-4R Agonist 1 | HS014 | [D-Trp8]-γ-MSH | (D-Phe7)-α-MSH | PG-931 | JKC363 | (-)-Isodocarpin | SHU 9119 | Adrenocorticotropic Hormone (ACTH) (1-39), rat | CCZ01048 TFA | β-Melanocyte Stimulating Hormone (MSH), human TFA | RO27-3225 TFA | γ-1-Melanocyte Stimulating Hormone (MSH), amide | ACTH (1-17) (TFA) | Terrein | γ1-MSH TFA
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货号: HY-10622
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