[CAS NO. 1351761-44-8]  GNE-7915

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PRODUCTS SPECIFICATIONS [1351761-44-8]

Catalog
SLK-S7528
Brand
Selleck
CAS
1351761-44-8

DESCRIPTION [1351761-44-8]

Overview

MDLMFCD25977005
Molecular Weight443.40
Molecular FormulaC19H21F4N5O3
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.2553 mL11.2765 mL22.5530 mL
5 mM0.4511 mL2.2553 mL4.5106 mL
10 mM0.2255 mL1.1276 mL2.2553 mL
50 mM---

Description

GNE-7915 is a highly potent, selective, and brain-penetrable inhibitor, with and of 9 nM and 1 nM, respectively.

Targets

LRRK2 [1]
(Cell-free assay)
LRRK2 [1]
(Cell-free assay)
1 nM(Ki)9 nM

In vitro

GNE-7915 is also a moderately potent 5-HT2B antagonist according to in vitro functional assays. GNE-7915 demonstrates excellent in vitro DMPK with minimal turnover in human hepatocytes.

In vivo

In rats, GNE-7915 demonstrates excellent in vivo PK profiles with long half-lives, good oral exposure and high passive permeability. GNE-7915 (50 mg/kg i.p. or p.o.) results in concentration-dependent knockdown of pLRRK2 in the brain of BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.