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Setmelanotide

CAS No. : 920014-72-8

MCE 站：Setmelanotide

产品活性：Setmelanotide (RM-493) 是一种黑皮质素 4 受体 (MC4R) 激动剂，作用于人和大鼠 MC4R，EC₅₀ 分别为 0.27 nM 和 0.28 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Melanocortin Receptor

In Vitro: Melanocortin receptor agonists act in the brain to regulate food intake and body weight and, independently of these actions. Setmelanotide exhibits agonist activity to human and rat MC4R with K_is of 2.1 and 2.7 nM and EC₅₀s of 0.27 and 0.28 nM, respectively.

In Vivo: Inhibition of refeeding after an overnight fast by BIM-22493 is dependent on functional MC4R, and does not require MC3R. BIM-22493 acutely improves glucose homeostasis. Lep^ob/Lep^ob mice treated with BIM-22493 exhibits significantly improved glucose clearance when compared to controls. Chronic BIM-22493 treatment was associated with significantly lower levels of serum glucose and HOMA-IR values. Treatment with setmelanotide results in transient decreases in food intake (35%), with persistent weight loss over 8 weeks of treatment (13.5%) in a diet-induced obese nonhuman primate model.

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