| 货号 | 1145/50 |
| 别名 | (2S,3S)-3-[[3,5-bis(Trifluoromethyl |
| 供应商 | Tocris |
| 生物活性 | Potent NK1 antagonist (Ki values are 0.08, 0.2 and 93.13 nM for gerbil, human and rat receptors, respectively). Produces anxiolytic-like effects in the gerbil elevated plus-maze. Exhibits antitumor activity in vitro. Also decreases HER2 activity and tumor growth in mice bearing HER2+ or EGFR+ breast tumors. Orally bioavailable and brain penetrant. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >99 % |
| 计算分子量 | 439.83 |
| 分子式 | C20H19F6NO.HCl |
| 可溶性/溶解性 | Soluble to 50 mM in water with gentle warming |
| CAS号 | 148700-85-0 |
| 参考文献 | Garcia-Recioet al (2013) Substance P autocrine signaling contributes to persistent HER2 activation that drives malignant progression and drug resistance in breast cancer. Cancer Res. 73 6424. PMID: 24030979. Vartyet al (2002) The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 27 371. PMID: 12225694. Krameret al (1998) Distinct mechanism for antidepressant blockade of central substance P receptors. Science 281 1640. PMID: 9733503. Seabrooket al (1996) L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Eur.J.Pharmacol. 317 129. PMID: 8982729. |