SB 218795是一种有效的选择性非肽 NK3 受体拮抗剂,对 hNK3 的 Ki 值为 13 nM,其对 hNK3 的选择性比 hNK2 和 hNK1 高 90 倍和 7000 倍。它能抑制 NK3 受体介导的兔瞳孔收缩。


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| 描述 | SB 218795 is a potent and selective non-peptide NK3 receptor antagonist with a Ki value of 13 nM for hNK3. SB 218795 is 90 and 7000 times more selective for hNK3 than hNK2 and hNK1, respectively. SB 218795 inhibits NK3 receptor-mediated pupil constriction in rabbits[1][2].In the concentration range of 3-30 nM, SB 218795 antagonises the contractile response induced by the NK3 receptor agonist Senktide in a surmountable concentration-dependent manner[2].At concentrations of 0.3-3 μM, SB 218795 does not affect the contractile response of the NK3 receptor agonist [MePhe7]-NKB in the rabbit iris sphincter[2]. |
| Animal study | Administered intravenously at doses of 0.25-1 mg/kg, SB 218795 inhibited Senktide-induced pupil constriction in rabbits with a maximum inhibition rate of 78%[2]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.61mL 2.52mL 1.26mL |
25.22mL 5.04mL 2.52mL |
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| CAS号 | 174635-53-1 |
| 分子式 | C25H20N2O3 |
| 分子量 | 396.44 |
| SMILES Code | O=C(OC)[C@@H](C1=CC=CC=C1)NC(C2=CC(C3=CC=CC=C3)=NC4=CC=CC=C24)=O |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | IUMQXQJZIHWLIN-HSZRJFAPSA-N |
| Pubchem ID | 6604858 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 250 mg/mL(630.62 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
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