MLi-2 - Moligand™, 10mM in DMSO , Inhibitor of leucine rich repeat kinase 2, CAS No.1627091-47-7, Inhibitor of leucine rich repeat kinase 2

CAS: 1627091-47-7 Cat. No.: M408789 Peso molecular: 379.46

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

1H-​Indazole, 3-​[6-​[(2R,​6S)​-​2,​6-​dimethyl-​4-​morpholinyl]​-​4-​pyrimidinyl]​-​5-​[(1-​methylcyclopropyl)​oxy]​-​, rel-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

MLi-2 MLi-2 is an orally active and highly selective inhibitor of LRRK2 . MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro with IC50 of 0.76 nM, a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 with IC50 o
In vitro

MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. 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.

In vivo

Acute oral and subchronic dosing in MLi-2 mice resulted in dosedependent 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 >100× the in vivo plasma IC50 for LRRK2 kinase inhibition as measured by pSer935 dephosphorylation. Morphologic changes in the lung, consistent with enlarged type II pneumocytes, are observed in MLi-2-treated MitoPark mice.
Cell Data

cell lines：U87-MG, T98G, and U373-MG

Concentrations：10 serial 3-fold dilutions, top concentration 5 μM

Incubation Time：90 min

Powder Purity:≥98%

Specifications

Sinónimos

1H-​Indazole, 3-​[6-​[(2R, ​6S)​-​2, ​6-​dimethyl-​4-​morpholinyl]​-​4-​pyrimidinyl]​-​5-​[(1-​methylcyclopropyl)​oxy]​-​, rel-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

MLi-2 is an orally active and highly selective inhibitor of LRRK2. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro with IC50 of 0.76 nM, a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 with IC50 of 1.4 nM,

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of leucine rich repeat kinase 2

Nombres e identificadores

• Isómeros SMILES: C[C@@H]1CN(C[C@@H](O1)C)C2=NC=NC(=C2)C3=NNC4=C3C=C(C=C4)OC5(CC5)C
• Peso molecular: 379.46
• Reaxy-Rn: 35816280
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=35816280&ln=

Objetivos asociados (humanos)

LRRK2 Tchem Leucine-rich repeat serine/threonine-protein kinase 2 (4 Activities)

Discover Target: LRRK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)