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Chemical Structure| 1351761-44-8 Chemical Structure| 1351761-44-8

Structure of GNE-7915
CAS No.: 1351761-44-8

Chemical Structure| 1351761-44-8

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GNE-7915 is a highly selective and brain-penetrant LRRK2 inhibitor with an IC50 value of 9 nM.

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Product Details of GNE-7915

CAS No. :1351761-44-8
Formula : C19H21F4N5O3
M.W : 443.40
SMILES Code : O=C(C1=CC(OC)=C(NC2=NC=C(C(F)(F)F)C(NCC)=N2)C=C1F)N3CCOCC3
MDL No. :MFCD25977005
InChI Key :XCFLWTZSJYBCPF-UHFFFAOYSA-N
Pubchem ID :58539171

Safety of GNE-7915

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • LRRK2

    LRRK2, Ki:1 nM

    LRRK2, IC50:9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
SH-SY5Y cells 0.1 to 100 nM 24 hours To assess the effect of GNE-7915 on αSyn phosphorylation, results showed significant reduction in pSer129-αSyn levels at doses of 1, 10, and 100 nM NPJ Parkinsons Dis. 2022 Sep 10;8(1):115
PD patient-derived lymphoblastoid cell lines (LCL) 1 μM 24 hours restore mtDNA damage to control levels Hum Mol Genet. 2017 Nov 15;26(22):4340-4351
primary rat midbrain neurons 0.5 nM 24 hours prevent or restore LRRK2 G2019S-induced mtDNA damage to control levels Hum Mol Genet. 2017 Nov 15;26(22):4340-4351

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice LRRK2R1441G mutant mouse model Subcutaneous injection 100 mg/kg Twice weekly for 18 weeks To evaluate the effect of long-term GNE-7915 treatment on αSyn oligomer accumulation, results showed significant reduction in striatal αSyn oligomers in mutant mice without causing peripheral adverse effects NPJ Parkinsons Dis. 2022 Sep 10;8(1):115

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.28mL

2.26mL

1.13mL

22.55mL

4.51mL

2.26mL

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