Ladostigil

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ladostigil (TV-3326) 是一种口服有效的胆碱酯酶 (cholinesterase) 和脑选择性单胺氧化酶 (MAO) 的双重抑制剂，抑制 MAO-B 和 AChE 的 IC50 值分别为 37.1 和 31.8 μM。Ladostigil 具有神经保护，抗氧化和抗炎的作用，可用于抑郁症和阿尔茨海默症的研究。Ladostigil 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease. Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Ladostigil (1-10 μM) exerts neuroprotective activities, including a prevention of the fall of the mitochondrial membrane potential (ψ), attenuation of apoptotic cascades and an inhibition of ROS production induced by OS insults.Ladostigil (1-10 μM) has a significant neuroprotective activity, including inhibition of caspase-3 activation, induction of Bcl-2 and reduction of Bad and Bax gene and protein expression in human neuroblastoma SK-N-SH cells.

Ladostigil (17 mg/kg; p.o. daily for 6 weeks) abolishes their hyperanxiety and depressive-like behaviour in the elevated plus maze (EPM) and forced swim tests (FST) tests in adulthood from puberty to prenatally-stressed rats.Ladostigil (50 μmol/kg; single p.o.) restores the loss of episodic memory in the object recognition test in rats.Animal Model:Pathogen-free (SPF) Sprague-Dawley ratsDosage:17 mg/kg Administration:P.o. (added to the drinking water) daily for 6 weeks Result:Inhibited brain MAO-A and B by more than 60%.Reduced hyperanxiety of male and female prenatally stressed (PS) rats in the EPM and depressive-like behaviour in the FST.

——

Metabolic Enzyme/Protease

MAO

MAO | Antioxidant | AChE

——

——

209394-27-4

272.34

C16H20N2O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (367.19 mM; 超声助溶 )

N(CC#C)[C@H]1C=2C(CC1)=CC=C(OC(N(CC)C)=O)C2

——

(-20℃)

With Ice Pack

≥ 2 years