Description References
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GNE-3511

Description References
GNE-3511 Structure
GNE-3511
  • CAS No.1496581-76-0
  • Chemical Name:GNE-3511
  • CBNumber:CB93146612
  • Molecular Formula:C23H26F2N6O
  • Formula Weight:440.49
  • MOL File:1496581-76-0.mol
GNE-3511 Property
  • Boiling point 579.0±50.0 °C(Predicted)
  • Density 1.37±0.1 g/cm3(Predicted)
  • storage temp. Store at -20°C
  • solubility DMSO:25.63(Max Conc. mg/mL);58.18(Max Conc. mM)
    Methanol:1.0(Max Conc. mg/mL);2.27(Max Conc. mM)
  • form A crystalline solid
  • pka 7.23±0.40(Predicted)
  • color Light yellow to yellow
  • UNSPSC Code 12352200
  • NACRES NA.77
Safety
  • HS Code  :2934999090
  • NFPA 704:
    0
    2 0
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501

GNE-3511 Chemical Properties,Usage,Production

  • Description GNE-3511 is a selective and highly potent inhibitor of dual leucine zipper kinase (DLK). It also inhibits phosphorylated JNKand is highly selective for DLK over other MAP kinases. In an MPTP mouse model of Parkinson’s disease, a high dose of GNE-3511 completely suppresses phosphorylated c-Jun (p-c-Jun) expression, while a low dose moderately reduces its expression. Study has also shown that GNE03511 displayed concentration-dependent protection of neurons from degeneration in vitro and demonstrated dose-dependent activity in two different animal models of disease. These results suggest that GNE-3511 may have therapeutic potential in multiple indications.
  • References Patel, S, et al. "Discovery of Dual Leucine Zipper Kinase (DLK, MAP3K12) Inhibitors with Activity in Neurodegeneration Models. " Journal of Medicinal Chemistry 58.1(2015):401-18.
    https://www.caymanchem.com/product/19174
  • Uses GNE-3511 is a potent and selective dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. GNE-3511 displays concentration-dependent protection of neurons from degeneration in vitro and demonstrated dose-dependent activity in two different animal models of disease. GNE-3511 displays protection of primary neurons in an in vitro axon degeneration assay as well as activity in the mouse models of glaucoma/optic neuropathy (optic nerve crush) and Parkinson’s disease (MPTP) after oral dosing.
  • Biological Activity Cell permeable: yes', 'Primary Target
    DLK', 'Reversible: yes
  • in vivo

    GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced nociceptive behavior by inhibiting DLK in mice[2].
    GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced edema and hemorrhage in mouse bladder[2].
    GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg) exhibits moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives, and brain penetration[2].
    Pharmacokinetic Parameters of GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg)[2].

    species CLp (mL/min/kgVdss (L/kgt1/2 (h)F (%)Bu/PuCSF/Pu
    mouse562.50.6450.24 at 6 h
    rat303.71.8630.70.4
    dog416.54320.4
    cynomolgous163.12.4190.6
    Animal Model:Cystitis mouse model[1]
    Dosage:75 mg/kg
    Administration:oral gavage;75 mg/kg; single
    Result:Significantly reduced the number of nociceptive behavior as well as nociceptive score.
    Had no impact on bladder weight, did not induce bladder edema or hemorrhage and significantly suppressed CYP-induced increase in bladder weight, bladder edema, and hemorrhage.
    Animal Model:mouse, rat, cynomolgus and dog[2]
    Dosage:1 mg/k, 5 mg/kg
    Administration:iv.; 1 mg/kg or po.; 5 mg/kg
    Result:Exhibited moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives and brain penetration.
GNE-3511 Preparation Products And Raw materials
Raw materials
Preparation Products
Global(82)Suppliers
  • Supplier:
    BOC Sciences
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  • Supplier:
    TargetMol Chemicals Inc.
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GNE-3511 Spectrum
1496581-76-0, GNE-3511Related Search:
  • API
  • 化学试剂
  • 抑制剂
  • 生物试剂
  • 细胞生物学试剂
  • C23H26F2N6O
  • 化合物GNE-3511,10 MM DMSO 溶液
  • 2-((6-(3,3-二氟吡咯烷-1-基)-4-(1-(氧杂环丁烷-3-基)哌啶-4-基)吡啶-2-基)氨基)异烟腈
  • 化合物GNE-3511
  • DLK/MAP3K12抑制剂(GNE-3511)
  • 1496581-76-0
  • DLK Inhibitor, GNE-3511
  • GNE-3511, 10 mM in DMSO
  • Inhibitor,MAP kinase kinase kinase, MEKK, MAPKKK,inhibit,neurodegenerative diseases,brain-penetrant,GNE 3511,MAP3K,GNE-3511,dual leucine zipper kinase (DLK),oral
  • GNE35Chemicalbook11
  • 4-Pyridinecarbonitrile, 2-[[6-(3,3-difluoro-1-pyrrolidinyl)-4-[1-(3-oxetanyl)-4-piperidinyl]-2-pyridinyl]amino]-
  • 2-((6-(3,3-DIFLUOROPYRROLIDIN-1-YL)-4-(1-(OXETAN-3-YL)PIPERIDIN-4-YL)PYRIDIN-2-YL)AMINO)ISONICOTINONITRILE
  • GNE3511;GNE 3511
  • CS-2506
  • 2-{[6-(3,3-DIFLUOROPYRROLIDIN-1-YL)-4-[1-(OXETAN-3-YL)PIPERIDIN-4-YL]PYRIDIN-2-YL]AMINO}PYRIDINE-4-CARBONITRILE
  • 2-[[6-(3,3-difluoropyrrolidin-1-yl)-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile
  • GNE-3511