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Netupitant-d6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Netupitant-d6图片
包装:1mg
规格:98%
市场价:3704元
分子量:584.6

产品介绍
Netupitant D6 是氘标记的 Netupitant (CID-6451149),它是一种高效和选择性的口服活性神经激肽-1 (NK1) 受体拮抗剂。
货号:ajcx20102
CAS:2070015-31-3
分子式:C30H26D6F6N4O
分子量:584.6
溶解度:DMSO: soluble,Methanol: soluble
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Netupitant-d6 is intended for use as an internal standard for the quantification of netupitant by GC- or LC-MS. Netupitant is an insurmountable antagonist of the neurokinin-1 (NK1) receptor (Ki = 0.95 nM in CHO cells expressing the human recombinant receptor).1 It is selective for human NK1 over human NK2 and NK3 and rat NK1 (Kis = >1,500 nM) and over 50 G protein-coupled receptors, monoamine transporters, and ion channels when used in the nanomolar range.2 Netupitant decreases the maximal response to substance P-induced contractions in isolated guinea pig ileum with long-lasting effects. It also dose-dependently inhibits the substance P-induced scratching, biting, and licking response in mice when used at doses ranging from 1 to 10 mg/kg and decreases NK agonist-induced foot tapping in gerbils (ID50s = 1.5 mg/kg, i.p., or 0.5 mg/kg, oral).


|1. Hoffmann, T., B•s, M., Stadler, H., 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. 16(5), 1362-1365 (2006).|2. Rizzi, A., Campi, B., Camarda, V., et al. In vitro and in vivo pharmacological characterization of the novel NK1 receptor selective antagonist Netupitant. Peptides 37(1), 86-97 (2012).