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 |
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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 性质
沸点 | 519.0±60.0 °C(Predicted) |
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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 |
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
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-13456 | LY-404187 | 1 mg | 400元 | |
2024/08/19 | HY-13456 | N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺 LY-404187 | 211311-95-4 | 5 mg | 1000元 |