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LY404187
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY404187图片
CAS NO:211311-95-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
LY404187 是一种有效、选择性和中枢活性的 AMPA 受体正变构调节剂,对 GluR1i、GluR2i、GluR2o、GluR3i 和 GluR4i 的 EC50 分别为 5.65、0.15、1.44、1.66 和 0.21 μM。
Cas No.211311-95-4
别名N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺
Canonical SMILESCC(CNS(C(C)C)(=O)=O)C(C=C1)=CC=C1C2=CC=C(C#N)C=C2
分子式C19H22N2O2S
分子量342.5
溶解度DMF: 15mg/mL,DMSO: 15mg/mL,DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL,Ethanol: 3mg/mL
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.1 It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 μM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 μM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 μM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.2,3 LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA in mouse and rat, respectively, models of Parkinson's disease when administered at a dose of 0.5 mg/kg per day.4

|1. Miu, P., Jarvie, K.R., Radhakrishnan, V., et al. Novel AMPA receptor potentiators LY392098 and LY404187: Effects on recombinant human AMPA receptors in vitro. Neuropharmacology 40(8), 976-983 (2001).|2. Baumbarger, P.J., Muhlhauser, M., Zhai, J., et al. Positive modulation of α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors in prefrontal cortical pyramidal neurons by a novel allosteric potentiator. J. Pharmacol. Exp. Ther. 298(1), 86-102 (2001).|3. Gates, M., Ogden, A., and Bleakman, D. Pharmacological effects of AMPA receptor potentiators LY392098 and LY404187 on rat neuronal AMPA receptors in vitro. Neuropharmacology 40(8), 984-991 (2001).|4. O'Neill, M.J., Murray, T.K., Whalley, K., et al. Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur. J. Pharmacol. 486(2), 163-174 (2004).