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BRL 54443

目录号: PL03277 纯度: ≥99%

BRL 54443 是 5-HT1E/1F 受体激动剂，Ki 分别为 1.1 nM 和 0.7 nM，比对其它 5-HT 和多巴胺受体的抑制性高 30 倍以上。

CAS No. :57477-39-1

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PL03277-10mg	10mg	¥562.00	请登录
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PL03277-100mg	100mg	¥2775.00	请登录
PL03277-200mg	200mg	¥3965.00	请登录
PL03277-10mM*1mLinDMSO	10mM*1mLinDMSO	¥1266.00	请登录
PL03277-1 mL x 10 mM (in DMSO)		¥388.00	请登录

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中文名称	BRL 54443
中文别名	3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇;3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇盐酸盐;5-羟基-3-(1-甲基哌啶-4-基)吲哚;BRL54443 抑制剂
英文名称	BRL 54443
英文别名	BRL 54443;BRL-54443;3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol;3-(1-Methylpiperidin-4-yl)-1H-indol-5-ol;5-hydroxy-3-(1-methylpiperidin-4-yl)indole;BRL 54443 HCl;3-(1-methylpiperidin-4-yl)1H-indol-5-ol;3-(1-methyl-piperidin-4-yl)-indol-5-ol;AC1L1DOE;Biomol-NT_000107;Lopac-B-173;Tocris-1129;UNII-Q2DH1CHI0Y;BRL54443;Q2DH1CHI0Y;1H-Indol-5-ol, 3-(1-methyl-4-piperidinyl)-;5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole;AK163730;5-Hydroxy-3-(1-methylpiperidine-4-yl)-1H-indole;Lopac0_000207;BPBio1_001401;GTPL3927;WKNFAD
Cas No.	57477-39-1
分子式	C₁₄H₁₈N₂O
分子量	230.31
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	BRL 54443 是 5-HT1E/1F 受体激动剂，Ki 分别为 1.1 nM 和 0.7 nM，比对其它 5-HT 和多巴胺受体的抑制性高 30 倍以上。

产品详情	BRL 54443 是 5-HT_1E/1F 受体激动剂，K_i 分别为 1.1 nM 和 0.7 nM，比对其它 5-HT 和多巴胺受体的抑制性高 30 倍以上。
生物活性	BRL 54443 is a potent 5-HT 1E/1F receptor agonist (K i values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.
性状	Solid
IC50 & Target[1][2]	5-HT1E Receptor 1.1 nM (Ki) 5-HT1F Receptor
体外研究(In Vitro)	Despite its low affinity for other receptors [5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT1F receptors. In DG membranes, BRL54443 selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production (IC50=14 nM). BRL 54443 also induces contraction (-log EC50=6.52). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats. 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	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Klein MT, et al. Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-867. [2]. McKune CM, et al. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (434.20 mM)配制储备液

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[1]. Klein MT, et al. Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-867.
[2]. McKune CM, et al. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.

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。

BRL 54443

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