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SB-616234-A

目录号: PL04889 纯度: ≥98%

SB-616234-A 是一种选择性的，可口服的 5-HT1B receptor 拮抗剂，具有抗焦虑和抗抑郁的功效。

CAS No. :908601-49-0

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中文名称	SB-616234-A
英文名称	SB-616234-A
英文别名	SB-616234A;SB 616234A;[6-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-5-methoxy-2,3-dihydroindol-1-yl]-[4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methanone;hydrochloride;1H-Indole, 6-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-2,3-dihydro-5-methoxy-1-[[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)[1,1′-biphenyl]-4-yl]carbonyl]-, monohydrochloride, rel- (9CI);SB 616234-A
Cas No.	908601-49-0
分子式	C₃₂H₃₆ClN₅O₃
分子量	574.11
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	SB-616234-A 是一种选择性的，可口服的 5-HT1B receptor 拮抗剂，具有抗焦虑和抗抑郁的功效。

产品详情	SB-616234-A 是一种选择性的，可口服的 5-HT1B receptor 拮抗剂，具有抗焦虑和抗抑郁的功效。
生物活性	SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
性状	Solid
IC50 & Target[1][2]	5-HT1B Receptor
体外研究(In Vitro)	SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pKi 6.6 ± 0.1). Similarly, affinity (pKi) for rat and guinea pig striatal 5-HT1B receptors is 9.2 ± 0.1. In [S]-GTPγS binding studies in the human recombinant cell line, SB-616234-A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [S]-GTPγS binding studies in rat striatal membranes, SB-616234-A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234-A (1 μM) potentiates electrically stimulated [H]-5-HT release from guinea pig a
体内研究(In Vivo)	SB-616234-A reverses the 5-HT1/7 receptor agonist, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED 50 of 2.4 mg/kg p.o. SB-616234-A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED 50 of 1.0 and 3.3 mg/kg i.p., respectively. SB-616234-A (0.3-30 mg/kg p.o.) causes a dose-dependent inhibition of ex vivo [H]-GR125743 binding to rat striatal 5-HT1B receptors with an ED 50 of 2.83 ± 0.39 mg/kg p.o. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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-[2methyl-4-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist. Neuropharma

溶解度数据	In Vitro: DMSO : 10 mg/mL (17.42 mM; Need ultrasonic)配制储备液

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[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-[2methyl-4-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist. Neuropharma

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

SB-616234-A

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