|N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺|CsnPharm

CAS No.: 211311-95-4

LY-404187 Catalog No. CSN22957

LY 404187 is a selective positive allosteric modulator of AMPA receptors with IC50s of 0.15, 0.21, 1.66 and 5.65 μM for GluA2i, GluA4i, GluA3i and GluA1i respectively.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY404187 potentiates the flip splice variant of these AMPA receptors to a greater degree than the flop splice variant. LY404187 has been shown to enhance glutamatergic synaptic transmission both in vitro and in vivo. LY404187 has been shown to enhance performance in animal models of cognitive function requiring different mnemonic processes^[1]. LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells^[1]. LY404187 is an extremely potent and centrally active potentiator of native AMPA receptors and has a unique mechanism of action. LY-404187 (0.03-10 µM) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC50=1.3±0.3 µM) and efficacy (Emax=45.3±8.0-fold increase). LY-404187 does not affect the magnitude or time course of wholecell K+ or Na+ currents in pre frontal cortex (PFC) pyramidal neurons at concentrations of 10 µM^[2]. LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent MPTP-induced neurotoxicity in mice. LY-404187 (0.5 mg/kg; s.c. for 28 days) attenuates apomorphine-induced contraversive rotations and affords significant protection against the loss of tyrosine hydroxylase positive nigral cell bodies. LY-404187 (0.1 or 0.5 mg/kg; s.c. for 14 days) affords functional, neurochemical and histological protection after infusion of 6-hydroxydopamine into the substantia nigra in rats. LY-404187 (0.5 mg/kg; s.c. for 14 days) delayed treatment provides functional and histological improvement, suggesting a trophic action as administration is initiated after cell death. LY-404187 (0.1 and 0.5 mg/kg; s.c. for 14 days) increases GAP-43 immunoreactivity in the striatum in a dose-dependent manner^[3].
参考文献

[1] Miu P, Jarvie KR, Radhakrishnan V, Gates MR, Ogden A, Ornstein PL, Zarrinmayeh H, Ho K, Peters D, Grabell J, Gupta A, Zimmerman DM, Bleakman D. Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. Neuropharmacology. 2001 Jun;40(8):976-83
[2] Baumbarger PJ, Muhlhauser M, Zhai J, Yang CR, Nisenbaum ES. Positive modulation of alpha-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. 2001 Jul;298(1):86-102
[3] O'Neill MJ, Murray TK, Whalley K, Ward MA, Hicks CA, Woodhouse S, Osborne DJ, Skolnick P. Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur J Pharmacol. 2004 Feb 20;486(2):163-74

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9201 mL
- 14.6004 mL
- 29.2009 mL
- 5 mM
- 0.5840 mL
- 2.9201 mL
- 5.8402 mL
- 10 mM
- 0.2920 mL
- 1.4600 mL
- 2.9201 mL

技术信息

CAS号	211311-95-4	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C19H22N2O2S	运输	蓝冰
分子量	342.46	别名

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

LY-404187 Catalog No. CSN22957

靶点选择性

请登录您的专属账户

确认信息