N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺

N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺

中文名称N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺
中文同义词N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺;N-[2-[4-(4-氰基苯基)苯基]丙基]丙烷-2-磺酰胺;N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺
英文名称N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide
英文同义词N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide;LY404187;N-(2-(4'-Cyano-[1,1'-biphenyl]-4-yl)propyl)propane-2-sulfonaMide;N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide;N-2-(4-(4-Cyanophenyl)phenyl)propyl-2-propanesulfonamide;LY-404187 N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide;CS-2739;100775
CAS号211311-95-4
分子式C19H22N2O2S
分子量342.46
EINECS号
相关类别
Mol文件211311-95-4.mol
结构式N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺 结构式

N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺 性质

沸点519.0±60.0 °C(Predicted)
密度1.19±0.1 g/cm3(Predicted)
储存条件Sealed in dry,Room Temperature
溶解度DMF:15 mg/ml;二甲基亚砜:15 mg/ml; DMSO:PBS (pH 7.2) (1:4):0.2mg/mL;乙醇:3 mg/ml
形态固体
酸度系数(pKa)11.24±0.40(Predicted)
颜色白色至米白色

N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺 用途与合成方法

LY-404187 是有效的,选择性和中枢活性的 AMPA 受体的正变构调节剂,作用于 GluR1i,GluR2i,GluR2o,GluR3i 和 GluR4i 的 EC50 值分别为 5.65、0.15、1.44、1.66 和 0.21 µM。LY-404187 有潜力用于许多精神疾病和神经退行性疾病的研究。

EC50: 5.65 µM (GluR1i), 0.15 µM (GluR2i), 1.44 µM (GluR2o), 1.66 µM (GluR3i), 0.21 µM (GluR4i)

LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells.
LY-404187 (0.03-10 µM) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC 50 =1.3±0.3 µM) and efficacy (E max =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.

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.

Animal Model: Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8
Dosage: 0.5 mg/kg
Administration: S.c; twice daily on weekdays and once daily at weekends for 11 days
Result: Attenuated the loss of tyrosine hydroxylase immunoreactivity in the substantia nigra.
No significant change in tyrosine hydroxylase immunoreactivity in the dorsal and ventral striatum.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-13456LY-4041871 mg400元
2024/04/30HY-13456N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺
LY-404187
211311-95-45 mg1000元

N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺 上下游产品信息

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