[CAS NO. 1536200-31-3] GNE-9605

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PRODUCTS SPECIFICATIONS [1536200-31-3]

Catalog

SLK-S7368

Brand

Selleck

CAS

1536200-31-3

DESCRIPTION [1536200-31-3]

Overview

MDL	-
Molecular Weight	449.83
Molecular Formula	C17H20ClF4N7O
SMILES	FC(C1=CN=C(NC2=C(Cl)N([C@@H]3[C@@H](F)CN(C4COC4)CC3)N=C2)N=C1NC)(F)F

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

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2231 mL	11.1153 mL	22.2306 mL
5 mM	0.4446 mL	2.2231 mL	4.4461 mL
10 mM	0.2223 mL	1.1115 mL	2.2231 mL
50 mM	0.0445 mL	0.2223 mL	0.4446 mL

Description

GNE-9605 is a highly potent and selective inhibitor with and of 2 nM and 19 nM, respectively.

Targets

LRRK2 ^[1]	LRRK2 ^[1]
2 nM(Ki)	19 nM

In vitro

GNE-9605 is highly potent against LRRK2 in both biochemical (Ki = 2.0 nM) and cellular (IC50 = 19 nM) assays. In vitro human MDR1 permeability data, GNE-9605 exhibits excellent brain penetration in higher species.

In vivo

In vivo rat PK studies with GNE-9605 (1 mg/kg, p.o.) demonstrates a total plasma clearance of 26 mL/min/kg with excellent oral bioavailability (90%). In BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation, GNE-9605 (10 and 50 mg/kg, i.p.) inhibits in vivo LRRK2 Ser1292 autophosphorylation.

References

[1] Estrada AA , et al. J Med Chem. 2014, 57(3), 921-936.