(Z)-SU4312 是 MAO-B 和 NOS 的抑制剂(IC50 值分别为 0.2 μM 和 19.0μM)。
半岛bd体育手机客户端 描述
(Z)-SU4312 is a inhibitor of MAO-B and NOS(IC50 value of 0.2 μM, 19.0μM,respectively).
体外活性
(Z)-SU4312 unexpectedly prevented MPP(+) -induced neuronal apoptosis in vitro and decreased MPTP-induced loss of dopaminergic neurons, reduced expression of mRNA for tyrosine hydroxylase and impaired swimming behaviour in zebrafish.?(Z)-SU4312 exhibited non-competitive inhibition of purified neuronal NOS (nNOS) with an IC(50) value of 19.0?μM but showed little or no effects on inducible and endothelial NOS. Molecular docking simulations suggested an interaction between (Z)-SU4312 and the haem group within the active centre of nNOS[1].
体内活性
(Z)-SU4312 was able to selectively inhibit monoamine oxidase-B (MAO-B) activity both in vitro and in vivo, with an IC50 value of 0.2 μM.(Z)-SU43122 provides therapeutic benefits in cellular and animal models of PD, possibly through multiple mechanisms including enhancement of MEF2D through the activation of PI3-K/Akt pathway, maintenance of mitochondrial biogenesis and inhibition of MAO-B activity.?(Z)-SU4312 thus may be an effective drug candidate for the prevention or even modification of the pathological processes of PD[2].
动物实验
MPP(+) -treated neurons and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated zebrafish were used to study neuroprotection by?(Z)-SU4312. NOS activity was assayed in vitro to examine direct interactions between?SU4312?and NOS isoforms[1].
Cas No.
90828-16-3
分子式
C17H16N2O
分子量
264.328
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years