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GYKI 53655 hydrochloride

AMPA和红藻氨酸受体拮抗剂,GYKI53655 hydrochloride 是 α-氨基-3-羟基-5-甲基异恶唑-4-丙酸 (AMPA) 的拮抗剂。

目录号: PC12284 纯度: ≥98%

CAS No. :143692-48-2

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中文名称	GYKI 53655 hydrochloride
英文名称	GYKI 53655 hydrochloride
英文别名	7H-1,3-Dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide,5-(4-aminophenyl)-8,9-dihydro-N,8-dimethyl-, hydrochloride (1:1);GYKI 53655 hydrochloride;1-(4-AMinophenyl)-3-MethylcarbaMyl-4-Methyl-3,4-dihydro-7,8-Methylenedioxy-5H-2,3-benzodiazepinehydrochloride;GYKI53655 hydrochloride;GYKI53655 HCl;7H-1,3-Dioxolo(4,5-h)(2,3)benzodiazepine-7-carboxamide, 8,9-dihydro-5-(4-aminophenyl)-N,8-dimethyl-, monohydrochloride;C19H20N4O3.HCl;Q27271407;1-(4-Aminophenyl)-3-methylcarbamyl- 4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride;1-(4-Aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methyle;LY-300168 MONOHYDROCHLORIDE;1-(4-Aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride;1-(4-Aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepinehydr;8,9-DIHYDRO-5-(4-AMINOPHENYL)-N,8-DIMETHYL-7H-1,3-DIOXOLO(4,5-H)(2,3)BENZODIAZEPINE- 7-CARBOXAMIDE HCL;JI4631600;Toxic solid, organic, n.o.s. (Buspirone hydrochloride);Toxic solid, organic, n.o.s. (GYKI 53655 hydrochloride)
Cas No.	143692-48-2
分子式	C₁₉H₂₁ClN₄O₃
分子量	388.85
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性	GYKI 53655 (LY300168) hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.
性状	Solid
IC50 & Target[1][2]	AMPA
体外研究(In Vitro)	GYKI 53655 (LY300168) hydrochloride inhibits α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 μM)-induced responses with IC₅₀ value of 5.9±0.1 μM. GYKI 53655 hydrochloride inhibits AMPA (10 μM) responses in recombinant G1uR4 expressing HEK293 cells with IC₅₀ value of 4.6±0.4 μM. Using 3 μM cyclothiazide the inhibition produced by GYKI 53655 hydrochloride is 79±2% (n=4 cells). GYKI 53655 hydrochloride produces only small inhibitions of kainate-induced currents at 30 μM and inhibits kainate-induced currents at a concentration of 100 μM by 12±2 (n=4) and 18±4 (n=4), respectively. GYKI 53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons with an IC₅₀ value of 1.5±0.1 μM. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	GYKI 53655 hydrochloride (4 mg/kg) is found to have a short-lasting depressant effect on neuronal responses to iontophoretic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), with a half-recovery time of approximately 7 min. GYKI 53655 hydrochloride (4 and 8 mg/kg) substantially depresses or completely abolishes AMPA responses. Results demonstrate the dose-dependence of GYKI 53655 hydrochloride (2 to 8 mg/kg) in depressing responses to AMPA. At the highest doses tested, GYKI 53655 hydrochloride reduces AMPA responses to a comparable degree. Tonic fit and death are completely prevented by GYKI 53655 hydrochloride at dose over 5.0 mg/kg. The ED₅₀ value of GYKI 53655 hydrochloride is 2.2 mg/kg i.p. The maximal effects of GYKI 53655 hydrochloride lasts 3 h then the exit inhibition effect of GYKI 53655 hydrochloride falls to 20% 1 h later. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature or refrigerated transportation.
储存方式	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Bleakman D, et al. Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors 体外研究: stereospecificity and selectivity profiles. Neuropharmacology. 1996;35(12):1689-702. [Information] [2]. Chizh BA, et al. A comparison of intravenous NBQX and GYKI 53655 as AMPA antagonists in the rat spinal cord. Br J Pharmacol. 1994 Jul;112(3):843-6. [Information] [3]. Szabados T, et al. Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res Bull. 2001 Jun;55(3):387-91. [Information]

溶解度数据

体外研究:

DMSO : ≥ 160 mg/mL (411.47 mM)

H₂O : 8 mg/mL (20.57 mM; Need ultrasonic and warming)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5717 mL	12.8584 mL	25.7169 mL
5 mM	0.5143 mL	2.5717 mL	5.1434 mL
10 mM	0.2572 mL	1.2858 mL	2.5717 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

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。

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