GNE-0877

CAS No. 1374828-69-9

GNE-0877( GNE0877 )

Catalog No. M11549 CAS No. 1374828-69-9

GNE-7915 is a highly potent, selective, brain-penetrating LRRK2 inhibitor with Ki of 0.6 nM (LRRK2 G2019S), pLRRK2 cell IC50 of 3 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 92 In Stock
2MG 52 In Stock
5MG 116 In Stock
10MG 187 In Stock
25MG 376 In Stock
50MG 551 In Stock
100MG 786 In Stock
200MG Get Quote In Stock
500MG 1609 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    GNE-0877
  • Note
    Research use only, not for human use.
  • Brief Description
    GNE-7915 is a highly potent, selective, brain-penetrating LRRK2 inhibitor with Ki of 0.6 nM (LRRK2 G2019S), pLRRK2 cell IC50 of 3 nM.
  • Description
    GNE-7915 is a highly potent, selective, brain-penetrating LRRK2 inhibitor with Ki of 0.6 nM (LRRK2 G2019S), pLRRK2 cell IC50 of 3 nM; induces abnormal cytoplasmic accumulation of secretory lysosome-related organelles known as lamellar bodies in type II pneumocytes of the lung in nonhuman primates, but no lysosomal abnormality in the kidney.
  • In Vitro
    GNE0877 (1 μM; 10-30 min) shows good cellular potency in human liver microsomes and hepatocytes.Cell Viability Assay Cell Line:Human liver microsomes and hepatocytes Concentration:1 μM Incubation Time:10, 20 and 30 min Result:Exibited low turnover and good vitro stability in human liver microsomes and hepatocytes with no glucuronidation.
  • In Vivo
    GNE0877 (10 and 50 mg/kg; i.p. once) inhibits LRRK2 Ser1292 autophosphorylation. Animal Model:BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation Dosage:10 and 50 mg/kg Administration:Intraperitoneal injection; 10 and 50 mg/kg once Result:Tration-dependently inhibited Ser1292 autophosphorylation with an IC50 of 3 nM.
  • Synonyms
    GNE0877
  • Pathway
    Autophagy
  • Target
    LRRK2
  • Recptor
    LRRK2
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    1374828-69-9
  • Formula Weight
    339.326
  • Molecular Formula
    C14H16F3N7
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 62 mg/mL (182.7 mM); Ethanol: <1 mg/mL; Water: <1 mg/mL ( < 1 mg/ml refers to the product slightly soluble or insoluble )
  • SMILES
    CC(N1N=C(C)C(NC2=NC=C(C(F)(F)F)C(NC)=N2)=C1)(C)C#N
  • Chemical Name
    2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile

Shipping & Storage Information

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

Reference

1. Fuji RN, et al. Sci Transl Med. 2015 Feb 4;7(273):273ra15.
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