CAS NO: | 2070015-31-3 |
包装: | 1mg |
市场价: | 3780元 |
Cas No. | 2070015-31-3 |
别名 | 奈妥吡坦 D6; CID-6451149-d6 |
Canonical SMILES | CN1CCN(C2=NC=C(N(C)C(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)C(C4=CC=CC=C4C)=C2)CC1 |
分子式 | C30H26D6F6N4O |
分子量 | 584.6 |
溶解度 | DMSO: soluble,Methanol: soluble |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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). |