化合物MAO-IN-M30二盐酸盐

生物活性靶点体外研究体内研究化合物MAO-IN-M30二盐酸盐试剂级价格

化合物MAO-IN-M30二盐酸盐

CAS号:64821-19-8
英文名:VAR10300 dihydrochloride
中文名:化合物MAO-IN-M30二盐酸盐
CBNumber:CB22750653
分子式:C14H15ClN2O
分子量:262.74
MOL File:64821-19-8.mol

化合物MAO-IN-M30二盐酸盐化学性质

储存条件 :2-8°C
溶解度 :DMSO, heptane and xylene: ≥21mg/mL
形态 :powder
颜色 :green-yellow
水溶解性 :Soluble to 100 mM in water

安全信息

危险品标志 :Xn
危险类别码 :22-41
安全说明 :26-39
WGK Germany :3

化合物MAO-IN-M30二盐酸盐性质、用途与生产工艺

生物活性 MAO-IN-M30 dihydrochloride 是一种口服活性，可通过血脑屏障的，脑选择性不可逆 MAO-A (IC50=37 nM) 和 MAO-B (IC50=57 nM) 抑制剂。MAO-IN-M30 dihydrochloride 是有效的铁螯合剂、自由基清除剂。MAO-IN-M30 dihydrochloride 对 Dexamethasone 诱导的脑细胞凋亡具有神经保护作用。MAO-IN-M30 dihydrochloride 在 MPTP 和 lactacystin 帕金森病模型中也显示出神经恢复活性。
靶点

MAO-A

37 nM (IC ₅₀ )

MAO-B

57 nM (IC ₅₀ )

体外研究

MAO-IN-M30 (0.25 nM; 72 hours) significantly increased cell viability to ~90% after exposure to Dexamethasone.
MAO-IN-M30 (0-10 μM; 24 hours) enhances PC12 cell survival.
MAO-IN-M30 treatment significantly decreases the occurrence of fragmented DNA compared to the dexamethasone-treated group in SH-SY5Y cells.

Cell Viability Assay

Cell Line:	SH-SY5Y cells
Concentration:	0.25 nM
Incubation Time:	72 hours
Result:	Significantly increased cell viability to ∼90% after exposure to Dexamethasone.

Cell Viability Assay

Cell Line:	PC12 cells
Concentration:	0-10 μM
Incubation Time:	24 hours
Result:	Enhanced the PC12 cell viability, the cell viability increasing to 85 ± 6 and 90 ± 7%.

体内研究

MAO-IN-M30 (0.5-2.5 mg/kg; p.o.; once daily for 14 consecutive days) possesses neuroprotective activities.

Animal Model:	Male C57/BL mice (20-22 g; MPTP-induced neurotoxicity in mice)
Dosage:	0.5, 2.5 mg/kg
Administration:	P.o.; once daily for 14 consecutive days
Result:	Significantly elevate striatal dopamine levels, reduce its metabolism, and elevate tyrosine-hydroxylase protein levels and activity. Elevated MPTP-reduced dopaminergic and transferrin receptor cell count in the SNpc.