1. Autophagy
  2. LRRK2
  3. MLi-2

MLi-2 

Cat. No.: HY-100411 Purity: 99.74%
Handling Instructions

MLi-2 est un inhibiteur oralement active et hautement sélectif de LRRK2 avec un IC50 de 0,76 nM. MLi-2 a le potentiel pour la maladie de Parkinson.

MLi-2 ist ein oral aktiver und hochselektiver LRRK2-Inhibitor mit einem IC50 von 0,76 nM. MLi-2 hat das Potenzial für die Parkinson-Krankheit.

MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.

For research use only. We do not sell to patients.

MLi-2 Chemical Structure

MLi-2 Chemical Structure

CAS No. : 1627091-47-7

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10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 276 In-stock
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50 mg USD 1176 In-stock
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100 mg USD 1980 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease[1].

IC50 & Target

IC50: 0.76 nM (LRRK2)[1]

In Vitro

MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro( IC50=0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50=1.4 nM), and a radioligand competition binding assay (IC50=3.4 nM). MLi-2 has greater than 295-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels[1].

In Vivo

Acute oral and subchronic dosing in MLi-2 mice results in dose-dependent central and peripheral target inhibition over a 24-hour period as measured by dephosphorylation of pSer935 LRRK2. Treatment of MitoPark mice with MLi-2 is well tolerated over a 15-week period at brain and plasma exposures. Morphologic changes in the lung, consistent with enlarged type II pneumocytes, are observed in MLi-2-treated MitoPark mice[1].

Molecular Weight

379.46

Formula

C₂₁H₂₅N₅O₂

CAS No.

1627091-47-7

SMILES

C[[email protected]@](C1)([H])O[[email protected]](C)([H])CN1C2=CC(C3=NNC4=CC=C(OC5(C)CC5)C=C43)=NC=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 60 mg/mL (158.12 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6353 mL 13.1766 mL 26.3532 mL
5 mM 0.5271 mL 2.6353 mL 5.2706 mL
10 mM 0.2635 mL 1.3177 mL 2.6353 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6 mg/mL (15.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice: MLi-2 is suspended in 30% Captisol and administered in a volume of 10 mL/kg. Dose calculations are on the basis of active moiety. Mice receive MLi-2 [1-100 mg/kg; by mouth (PO)], or vehicle 1 hour prior to euthanasia by excess CO2. Immediately following euthanasia, mouse brain cortex is dissected and frozen on a steel plate over dry ice for analysis of pSer935 LRRK2 via Western Blot. Plasma and brain samples are collected and frozen for determination of MLi-2 levels by LC-MS/MS[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.74%

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Keywords:

MLi-2MLi2MLi 2LRRK2Leucine-rich repeat kinase 2orallyParkinson’sdiseaseInhibitorinhibitorinhibit

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MLi-2
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