Ladostigil

CAS No. 209394-27-4

Ladostigil( —— )

Catalog No. M34636 CAS No. 209394-27-4

Ladostigil (Ladostigil free base) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) with inhibitory effects on MAO-B and AChE, with IC50 values of 37.1 and 31.8 μM, respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Ladostigil
  • Note
    Research use only, not for human use.
  • Brief Description
    Ladostigil (Ladostigil free base) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) with inhibitory effects on MAO-B and AChE, with IC50 values of 37.1 and 31.8 μM, respectively.
  • Description
    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.
  • In Vitro
    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.
  • In Vivo
    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.
  • Synonyms
    ——
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    MAO
  • Recptor
    MAO | Antioxidant | AChE
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    209394-27-4
  • Formula Weight
    272.34
  • Molecular Formula
    C16H20N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (367.19 mM; Ultrasonic )
  • SMILES
    N(CC#C)[C@H]1C=2C(CC1)=CC=C(OC(N(CC)C)=O)C2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Denya I, et, al. Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease. Medchemcomm. 2018 Jan 16; 9(2):357-370.?
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