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713121-80-3

中文名稱(chēng) ML193
英文名稱(chēng) 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 2024/09/04 09:32:07
713121-80-3 結(jié)構(gòu)式 713121-80-3 結(jié)構(gòu)式

基本信息

中文別名
N-(4-(N-(3,4-二甲基異惡唑-5-基)氨磺?;?苯基)-6,8-二甲基-2-(吡啶-2-基)喹啉-4-甲酰胺
英文別名
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)-

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度≤0.1mg/ml in ethanol;2mg/ml in DMSO;3mg/ml in dimethyl formamide
形態(tài)結(jié)晶固體
顏色Off-white to yellow

常見(jiàn)問(wèn)題列表

生物活性
ML-193 (CID 1261822) 是一種有效和選擇性的 GPR55 拮抗劑,IC50 值為 221 nM。ML-193 對(duì) GPR55 的選擇性是 GPR35,CB1 和 CB2 的 27 倍以上。ML-193 可以改善帕金森氏病 (PD) 大鼠的運(yùn)動(dòng)和感覺(jué)運(yùn)動(dòng)缺陷。
靶點(diǎn)

IC50: 221 nM (GPR55)

體外研究

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.

體內(nèi)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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