HG-10-102-01 --- LRRK2 Inhibitor


Catalog No. size PriceQuantity
M60061-2D 10 mM in DMSO (0.529 mL) $139
M60061-2S 2mg solid $139
M60061-10S 10 mg solid $549

Description

HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant (IC50 for LRRK2-wild-type ~20.3 nM and LRRK2-[G2019S] ~3.2 nM). It significantly inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1−0.3 μM in cells. HG-10-102-01 is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg. It may represent a good lead compound for a subset of Parkinson's disease.

Product information

CAS Number: 1351758-81-0

Molecular Weight: 377.83

Formula: C17H20ClN5O3

Chemical Name: (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone

Smiles: COC1=CC(=CC=C1NC1=NC(NC)=C(Cl)C=N1)C(=O)N1CCOCC1

InChiKey: YEVOZZZLKJKCCD-UHFFFAOYSA-N

InChi: InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4,9-10H,5-8H2,1-2H3,(H2,19,20,21,22)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

HG-10-102-01was used at 0.3-1.0 µM final concentration in vitro and in cellular assays.

In Vivo:

HG-10-102-01 was intraperitoneally (IP) dosed to mice at 50 mg/kg once per day.

References:

  1. Choi HG, et al. Brain Penetrant LRRK2 Inhibitorn (2012) ACS Med. Chem. Lett., 2012, 3 (8), 658–662.
  2. Chen H, et al. Discovery of Selective LRRK2 Inhibitors Guided by Computational Analysis and Molecular Modeling. (2012) Journal of Medicinal Chemistry. 55(11), 5536-5545.

Products are for research use only. Not for human use.


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