GNE-9605

CAS No. 1536200-31-3

GNE-9605( GNE9605 | GNE 9605 )

Catalog No. M12169 CAS No. 1536200-31-3

GNE-9605 is a highly potent, selective, brain penetrant LRRK2 inhibitor with Ki of 2 nM, pLRRK2 IC50 of 19 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 49 In Stock
5MG 80 In Stock
10MG 147 In Stock
25MG 300 In Stock
50MG 444 In Stock
100MG 659 In Stock
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Biological Information

  • Product Name
    GNE-9605
  • Note
    Research use only, not for human use.
  • Brief Description
    GNE-9605 is a highly potent, selective, brain penetrant LRRK2 inhibitor with Ki of 2 nM, pLRRK2 IC50 of 19 nM.
  • Description
    GNE-9605 is a highly potent, selective, brain penetrant LRRK2 inhibitor with Ki of 2 nM, pLRRK2 IC50 of 19 nM; dispalys excellent selectivity against 178-membered Invitrogen kinase panel, as well as a representative panel of receptors and ion channels; demonstrates robust concentration-dependent inhibition of LRRK2 Ser1292 autophosphorylation (IC50=20 nM) in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
  • In Vitro
    ——
  • In Vivo
    GNE-9605 (10 and 50 mg/kg; i.p.; once) inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein.GNE-9605 (1 mg/kg, p.o.; 0.5 mg/kg, i.v.; once) displays LRRK2 Ki in the biochemical assay of 2 nM as well as a cellular IC50 of 19 nM. GNE-9605 has a total plasma clearance with excellent oral bioavailability. Animal Model:BAC transgenic mice expressing human LRRK2 protein.Dosage:10 and 50 mg/kg Administration:Intraperitoneal injection; once Result:Inhibited LRRK2 Ser1292 autophosphorylation in a dose-dependent manner.Animal Model:BAC transgenic mice expressing human LRRK2 protein.Dosage:1 mg/kg, p.o.; 0.5 mg/kg, i.v.Administration:Oral administration and intravenous injection; once Result:Demonstrated a total plasma clearance of 26 mL min-1 kg-1 with excellent oral bioavailability (90%).
  • Synonyms
    GNE9605 | GNE 9605
  • Pathway
    Autophagy
  • Target
    LRRK2
  • Recptor
    LRRK2
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    1536200-31-3
  • Formula Weight
    449.8336
  • Molecular Formula
    C17H20ClF4N7O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 60 mg/mL
  • SMILES
    FC(C1=CN=C(NC2=C(Cl)N([C@H]3[C@H](F)CN(C4COC4)CC3)N=C2)N=C1NC)(F)F
  • Chemical Name
    2,4-Pyrimidinediamine, N2-[5-chloro-1-[(3R,4R)-3-fluoro-1-(3-oxetanyl)-4-piperidinyl]-1H-pyrazol-4-yl]-N4-methyl-5-(trifluoromethyl)-, rel-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Estrada AA, et al. J Med Chem. 2014 Feb 13;57(3):921-36.
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