Velneperit

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Chemical Structure| 342577-38-2 同义名 : S2367
CAS号 : 342577-38-2
货号 : A533511
分子式 : C17H24F3N3O3S
纯度 : 99%+
分子量 : 407.451
MDL号 : MFCD11973642
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(73.63 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Neuropeptide Y (NPY), an amino acid, used for various physiological processes for management and treatment of various ailments related to central nervous system, cardiovascular system, respiratory system, gastro-intestinal system and endocrinal system[2].NPY displays a multiplicity of physiological effects that are transmitted by at least six G-protein coupled receptors (GPCRs) named Y(1), Y(2), Y(3), Y(4), Y(5), and y(6)[3]. NPY has also been shown to interact with sigma receptor in vivo and in vitro. There are indications that more subtypes might exist. Ligand binding studies reveal that Y1, Y2 and Y3 receptors are all G-protein coupled[4]. Among them, the Y5 receptor subtype is thought to play a role in meal initiation and the regulation of energy balance. Therefore, an antagonist of the NPY Y5 receptor is considered to have potential as an antiobesity drug[5]. Velneperit is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist[1]. It has been shown to have a significant effect on weight loss in clinical studies, suggesting its potential as a promising antiobesity drugKawanishi, Y.; Takenaka, H.; Hanasaki, K.; Okada, T.WO0137826A1.. In addition, it can ameliorate the glucose metabolism, reduce LDL cholesterol and uric acid levels, lower blood pressure, and improve liver functionKobayashi, Y.; Yoshioka, Y. WO2013002313A1..
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.54mL

4.91mL

2.45mL
参考文献

[1] Shinichi Oda*, et al. Development of an Optimized Synthetic and Purification Process of S-2367 (Velneperit), a Novel Neuropeptide Y (NPY) Y5 Receptor Antagonist. Org. Process Res. Dev., 2015, 19 (4), pp 531-536.

[2] Pravin Shende,et al. Physiological and Therapeutic Roles of Neuropeptide Y on Biological Functions. Adv Exp Med Biol. 2020;1237:37-47.

[3] A Bettio,et al. Biophysical methods to study ligand-receptor interactions of neuropeptide Y. Biopolymers. 2001;60(6):420-37.

[4]C P Wan,et al. Neuropeptide Y receptor subtypes. Life Sci. 1995 Feb 17;56(13):1055-64.

[5] Levens, N. R.; Della-Zuana, Neuropeptide Y Y5 receptor antagonists as anti-obesity drugs.Current Opinion in Investigational Drugs, 01 Oct 2003, 4(10):1198-1204.