| Description | SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1. |
| In vitro | SB 218795（3-30 nM）以一种可克服和浓度依赖性方式拮抗由senktide引起的收缩反应[1]。 |
| In vivo | 在兔子身上，SB 218795 (0.25-1 mg/kg; i.v.) 通过最大抑制率达到78%[1]，抑制了NK3受体介导的瞳孔收缩。 |
| Target activity | NK3 (human):13 nM (Ki), NK2 (human):1220 nM (Ki) |
| molecular weight | 396.44 |
| Molecular formula | C25H20N2O3 |
| CAS | 174635-53-1 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 5 mM DMSO: 60 mg/mL (151.35 mM) |
| References | 1. Medhurst AD, et, al. In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br J Pharmacol. 1997 Oct;122(3):469-76. 2. Valero MS, et, al. Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin. 2011 Apr;32(4):487-94. 3. Giardina GA, et, al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J Med Chem. 1997 Jun 6;40(12):1794-807. |