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Netupitant

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Chemical Structure| 290297-26-6 同义名 : CID 6451149;Ro 67-31898/000
CAS号 : 290297-26-6
货号 : A913871
分子式 : C30H32F6N4O
纯度 : 98%
分子量 : 578.592
MDL号 : MFCD25976831
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 8 mg/mL(13.83 mM)，配合低频超声，并水浴加热至45℃助溶，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 Neurokinin (NK) receptors belong to the family of G-protein coupled receptors and can be divided into three subtypes: NK1, NK2 and NK3. The endogenous ligand for NK1 receptor is the 11 amino acid neuropeptide substance P (SP)[3]. Netupitant is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM[3]. In CHO NK1 cells, netupitant concentration-dependently antagonized the stimulatory effects of substance P (SP) showing insurmountable antagonism (pK(B) 8.87)[4]. In the guinea pig ileum, netupitant concentration-dependently depressed the maximal response to SP (pK(B) 7.85) and, in functional washout experiments, displayed persistent (up to 5h) antagonist effects. In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that was dose-dependently inhibited by netupitant given intraperitoneally in the 1-10 mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1 agonist was dose-dependently counteracted by netupitant given intraperitoneally (ID(50) 1.5mg/kg) or orally (ID(50) 0.5mg/kg)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.64mL

1.73mL

0.86mL

17.28mL

3.46mL

1.73mL
参考文献

[1]Stathis M, Pietra C, et al. Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects. Eur J Pharmacol. 2012 Aug 15;689(1-3):25-30.

[2]Hoffmann T, Bos M, et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. Epub 2005 Dec 5.

[3]Hoffmann T, Bös M, Stadler H, Schnider P, Hunkeler W, Godel T, Galley G, Ballard TM, Higgins GA, Poli SM, Sleight AJ. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. doi: 10.1016/j.bmcl.2005.11.047. Epub 2005 Dec 5. PMID:16332435.

[4]Rizzi A, Campi B, Camarda V, Molinari S, Cantoreggi S, Regoli D, Pietra C, Calo' G. In vitro and in vivo pharmacological characterization of the novel NK₁ receptor selective antagonist Netupitant. Peptides. 2012 Sep;37(1):86-97. doi: 10.1016/j.peptides.2012.06.010. Epub 2012 Jun 23. PMID: 22732666.