| 货号 | 14867-1mg |
| 描述 | Substance P, a neurokinin peptide found in the brain and gastrointestinal tract, is thought to modulate stress responses, including the emetic reflex. Its actions are mediated through the neurokinin-1 (NK1) receptor, one of three GPCRs that couple neurokinin binding to the inositol phosphate signal transduction pathway.1,2 Aprepitant is an anti-emetic compound that selectively antagonizes the human NK1 receptor (Kis = 3 and 454.1 nM for hNK1 and hNK3, respectively; IC50 = 0.09 nM for hNK1).1,2Inin vivo assays to measure peripheral (guinea pig SYVAL assay) and central (gerbil foot-tapping stress response assay) inhibition of NK1 receptors, aprepitant demonstrates ED50 values of 0.008 and 0.36 mg/kg, respectively.3 Through antagonism of NK1 receptor activity, aprepitant has found clinical use to prevent chemotherapy-induced nausea and vomiting.4 |
| 别名 | Emend;L-754,030;MK-869;ONO-7436; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bissantz, C.,Bohnert, C.,Hoffmann, T., et al. Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonists. Journal of Medicinal Chemistry 55(11), 5061-5076 (2012). 2.Finke, P.E.,Meurer, L.C.,Levorse, D.A., et al. Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR. Bioorganic & Medicinal Chemistry Letters 16(17), 4497-4503 (2006). 3.Meurer, L.C.,Finke, P.E.,Owens, K.A., et al. Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives. Bioorganic & Medicinal Chemistry Letters 16(17), 4504-4511 (2006). 4.Hesketh, P.J.,Grunberg, S.M.,Gralla, R.J., et al. The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: A multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin-The aprepitant protocol 052 study group. Journal of Clinical Oncology 21(22), 4112-4119 (2003). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 534.4 |
| 分子式 | C23H21F7N4O3 |
| CAS号 | 170729-80-3 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |