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SB 242084 Sale

(Synonyms: 6-氯-2,3-二氢-5-甲基-N-[6-[(2-甲基-3-吡啶基)氧]-3-吡啶基]-1H-吲哚-1-酰胺盐酸盐) 目录号 : GC14392

Specific antagonist of 5-HT2C

SB 242084 Chemical Structure

Cas No.:181632-25-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥990.00
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1mg
¥409.00
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5mg
¥900.00
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10mg
¥1,125.00
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25mg
¥1,796.00
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50mg
¥2,664.00
现货
100mg
¥3,960.00
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Sample solution is provided at 25 µL, 10mM.

Description

SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

References:
[1]. Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
[2]. Bromidge SM, et al. 6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist. J Med Chem. 1997 Oct 24;40(22):3494-6.
[3]. Dalton GL, et al. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology (Berl). 2006 Mar;185(1):45-57.

化学性质

Cas No. 181632-25-7 SDF
别名 6-氯-2,3-二氢-5-甲基-N-[6-[(2-甲基-3-吡啶基)氧]-3-吡啶基]-1H-吲哚-1-酰胺盐酸盐
化学名 6-chloro-5-methyl-N-(6-((2-methylpyridin-3-yl)oxy)pyridin-3-yl)indoline-1-carboxamide
Canonical SMILES CC1=CC2=C(C=C1Cl)N(C(NC3=CN=C(C=C3)OC4=C(C)N=CC=C4)=O)CC2
分子式 C21H19ClN4O2 分子量 394.85
溶解度 ≥ 39.5mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

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1 mg 5 mg 10 mg
1 mM 2.5326 mL 12.663 mL 25.3261 mL
5 mM 0.5065 mL 2.5326 mL 5.0652 mL
10 mM 0.2533 mL 1.2663 mL 2.5326 mL
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