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713121-80-3

中文名称 ML193
英文名称 ML193
CAS 713121-80-3
分子式 C28H25N5O4S
分子量 527.59
MOL 文件 713121-80-3.mol
更新日期 2023/03/20 15:41:25
713121-80-3 结构式 713121-80-3 结构式

基本信息

中文别名
N-(4-(N-(3,4-二甲基异恶唑-5-基)氨磺酰基)苯基)-6,8-二甲基-2-(吡啶-2-基)喹啉-4-甲酰胺
英文别名
ML193
ML193 trifluoroacetate >=98% (HPLC)
N-[4-[[(3,4-Dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide
4-Quinolinecarboxamide, N-[4-[[(3,4-dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-

物理化学性质

储存条件-20°C储存
溶解度≤0.1mg/ml in ethanol;2mg/ml in DMSO;3mg/ml in dimethyl formamide
形态结晶固体

常见问题列表

生物活性
ML-193 (CID 1261822) 是一种有效和选择性的 GPR55 拮抗剂,IC50 值为 221 nM。ML-193 对 GPR55 的选择性是 GPR35,CB1 和 CB2 的 27 倍以上。ML-193 可以改善帕金森氏病 (PD) 大鼠的运动和感觉运动缺陷。
靶点

IC50: 221 nM (GPR55)

体外研究

ML-193 (0.01-100 μM; pretreated for 15 min) inhibits β-arrestin trafficking induced by L-α-lysophophosphatidylinositol (LPI, 10 μM) and ML186 (1 μM) with IC 50 s of 0.22 μM and 0.12 μM, respectively.
ML-193 (0.01-10 μM; pretreated for 30 min) decreases the LPI-mediated ERK1/2 phosphorylation, with an IC 50 of 0.2 μM in U2OS cells.
ML-193 (5 μM; pretreated for 30 min) attenuates the GPR55 agonists induced increases in hNSCs proliferation rates.
ML-193 (5 μM; 10 d) attenuates the ML184-induced increases in hNSCs differentiation.

体内研究

ML193 (1 and 5 µg/rat; intra-striatal at a rate of 1 μL/min) attenuates sensorimotor deficits and slip steps, increases motor coordination in PD rats.

Animal Model: Male Wistar rats (200-250 g) were induced experimental Parkinson by 6-hydroxydopamine (6-OHDA, 10 µg/rat)
Dosage: 1 and 5 µg/rat
Administration: Injected into the right striatum at a rate of 1 μL/min
Result: Increased the time on the rotarod, decreased latency to remove the label and slip steps in 6-OHDA-lesioned rats.
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