GNE-9605

SKU: orb1307478

Description

GNE-9605 is a potent and selective brain-penetrant inhibitor of LRRK2 kinase, exhibiting an IC50 of 19 nM. It is a valuable research tool for investigating LRRK2's role in Parkinson's disease, suitable for both cellular assays and in vivo models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1536200-31-3
• MW: 449.83
• Purity: 98.55%
• Formula: C₁₇H₂₀ClF₄N₇O
• SMILES: CNc1nc(Nc2cnn([C@H]3CCN(C[C@@H]3F)C3COC3)c2Cl)ncc1C(F)(F)F
• Target: LRRK2
• Solubility: Ethanol:10 mg/mL (22.23 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:82 mg/mL (182.29 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.34 mM)

Bioactivity

• Target IC50:
  LRRK2:19 nM
• In Vivo:
  In vitro human MDR1 permeability data indicate that GNE-9605 exhibits favorable brain penetration in higher organisms. In biochemical (Ki: 2.0 nM) and cellular (IC50: 19 nM) assays, GNE-9605 demonstrates potent inhibitory activity against LRRK2.
• In Vitro:
  In rats, PKGNE-9605 administered orally at a dose of 1 mg/kg exhibited a total plasma clearance rate of 26 mL/min/kg, achieving an oral bioavailability of 90%. In BAC transgenic mice models expressing the human LRRK2 G2019S mutation associated with Parkinson's disease, GNE-9605, administered intraperitoneally at doses of 10 and 50 mg/kg, was able to inhibit the autophosphorylation of LRRK2 at Ser1292.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Parkinson's disease, oral bioavailability, LRRK2 Ser1292, LRRK2, inhibit, GNE9605, GNE-9605, GNE 9605, Inhibitor, Leucine-rich repeat kinase 2, autophosphorylation

Compound Identifiers

PubChem CID

76328936