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SB 218795

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Chemical Structure| 174635-53-1 同义名 : -
CAS号 : 174635-53-1
货号 : A1209207
分子式 : C25H20N2O3
纯度 : 97%
分子量 : 396.438
MDL号 : -
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
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].
实验方案
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
参考文献

[1]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.

[2]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.