SB-616234-A

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Chemical Structure| 908601-49-0 同义名 : -
CAS号 : 908601-49-0
货号 : A1177339
分子式 : C32H36ClN5O3
纯度 : 98%
分子量 : 574.113
MDL号 : MFCD31382381
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(15.68 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-616234-A is distinguished by its high affinity for 5-HT1B receptors in CHO cells expressing the human variant (pKi 8.3 ± 0.2), displaying significant selectivity over other molecular targets except h5-HT1D receptors (pKi 6.6 ± 0.1). Its affinity for 5-HT1B receptors from rat and guinea pig striatum is high (pKi 9.2 ± 0.1). In binding studies using [35S]-GTPγS in a human recombinant cell line, SB-616234-A functions as a potent antagonist (pA2 value of 8.6 ± 0.2) without showing any agonistic activity. Similar antagonist activity is observed in rat striatal membranes (apparent pKB of 8.4 ± 0.5). At a concentration of 1 μM, SB-616234-A enhances electrically evoked [^3H]-5-HT release from cortical slices of guinea pig and rat brains, increasing the S2/S1 ratios to 1.8 and 1.6, respectively[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.71mL

1.74mL

0.87mL

17.42mL

3.48mL

1.74mL
参考文献

[1]Lee A.Dawson, et al. Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): In

[2]Scott C, et al. SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'methyl-4'-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist. Neuropharma