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CAS No. : 1496581-76-0
MCE 国际站:GNE-3511
产品活性:GNE-3511 是一种生物可利用性和脑渗透 dual leucine zipper kinase (DLK) 抑制剂,具有口服活性,其 Ki 值为 0.5 nM。GNE-3511 可穿过血脑屏障,被用于神经退行性疾病的研究。
研究领域:MAPK/ERK Pathway
作用靶点:MAP3K
In Vitro: GNE-3511 has inhibitory activity for p-JNK and DRG with IC50 values of 30 nM and 107 nM, respectively.
GNE-3511 has kinase selectivity for MKK4, MKK7, JNK1, JNK2, JNK3, MLK1, MLK2 and MLK3 with IC50 values of >5000 nM, >5000 nM, 129 nM, 514 nM, 364 nM, 67.8 nM, 767 nM and 602 nM, respectively.
GNE-3511 displays concentration-dependent protection of neurons from degeneration in vitro.
In Vivo: GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced nociceptive behavior by inhibiting DLK in mice.
GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced edema and hemorrhage in mouse bladder.
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.
Pharmacokinetic Parameters of GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg).
species | CLp (mL/min/kg | Vdss (L/kg | t1/2 (h) | F (%) | Bu/Pu | CSF/Pu |
mouse | 56 | 2.5 | 0.6 | 45 | 0.24 at 6 h | |
rat | 30 | 3.7 | 1.8 | 63 | 0.7 | 0.4 |
dog | 41 | 6.5 | 4 | 32 | | 0.4 |
cynomolgous | 16 | 3.1 | 2.4 | 19 | | 0.6 |
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | CNS-Penetrant Compound Library | Oxygen Sensing Compound Library | Orally Active Compound Library | Chemical Probe Library | Neurodegenerative Disease-related Compound Library | Anti-Obesity Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | TAO Kinase inhibitor 1 | ASK1-IN-4 | ASK1-IN-2 | NQDI-1 | GS-444217 | Tpl2 Kinase Inhibitor 1 | AZ-TAK1 | TAK1-IN-2 | Takinib | Selonsertib | Cot inhibitor-1 | SM1-71 | TAK1/MAP4K2 inhibitor 1 | DDO3711 | TAK1-IN-4 | PF-05381941 | GNE-8505 | Cot inhibitor-2 | ASK1-IN-3 | DLK-IN-1 | 5Z-7-Oxozeaenol | SW083688 | 7,3',4'-Trihydroxyisoflavone | TC ASK 10 | TAK1-IN-3 | NG25
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货号: HY-12947
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