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1031602-63-7

中文名称 UNC3230
英文名称 UNC3230
CAS 1031602-63-7
分子式 C17H20N4O2S
分子量 344.43
MOL 文件 1031602-63-7.mol
更新日期 2024/07/23 09:41:47
1031602-63-7 结构式 1031602-63-7 结构式

基本信息

中文别名
化合物UNC 3230
5-(环己烷甲酰胺基)-2-(苯基氨基)噻唑-4-甲酰胺
英文别名
UNC3230
5-[(Cyclohexylcarbonyl)amino]-2-(phenylamino)-thiazolecarboxamide
2-anilino-5-(cyclohexanecarbonylamino)-1,3-thiazole-4-carboxamide
4-Thiazolecarboxamide, 5-[(cyclohexylcarbonyl)amino]-2-(phenylamino)-

物理化学性质

储存条件-20°C储存
溶解度DMSO:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
Ethanol:0.2(Max Conc. mg/mL);0.58(Max Conc. mM)
形态结晶固体
颜色Off-white to light yellow

图谱信息

常见问题列表

生物活性
UNC3230 是一种有效的选择性的,ATP 竞争性的磷脂酰肌醇 4 磷酸 5 激酶 1C 型 (PIP5K1C) 抑制剂,IC50 约为 41 nM。UNC3230 还可抑制 PIP4K2C,但不抑制其他调节磷酸肌醇水平的脂质激酶。UNC3230 具有镇痛和抗癌作用。
靶点

IC50: ~41 nM (Phosphatidylinositol 4-phosphate 5 kinase type 1C (PIP5K1C))

体外研究

Membrane PIP2 levels are significantly reduced by ~45% in dorsal root ganglia (DRG) neurons treated with 100 nM UNC3230 (~2-fold above the IC50) relative to vehicle controls. UNC3230 significantly reduces lysophosphatidic acid (LPA)-evoked calcium signaling in cultured DRG neurons relative to vehicle.

体内研究

UNC3230 (2 nmol) significantly increases noxious heat-evoked paw withdrawal latency for two hours after intrathecal injection in wild-type mice, indicating an antinociceptive effect.
UNC3230 (2 nmol; intrathecal injection) is administered then one hour later co-injected 1 nmol LPA with UNC3230 (2 nmol, intrathecal injection). UNC3230 significantly blunts thermal hyperalgesia and mechanical allodynia compared to vehicle.
UNC3230 (2 nmol; intrathecal injection) significantly blunts thermal hyperalgesia and mechanical allodynia in the complete Freund’s adjuvant (CFA)-inflamed hindpaw (relative to vehicle control) but does not affect thermal or mechanical sensitivity in the control (non-inflamed) hindpaw over a multiday time course.

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