产品
编 号：F175475
分子式：C23H26F2N6O
分子量：440.49
分子式：C23H26F2N6O
分子量：440.49
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 1496581-76-0
产品详情
生物活性：
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.
体内研究：
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 plasmaclearances, 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/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
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
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.
体外研究：
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.
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.
体内研究：
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 plasmaclearances, 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/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
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
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.
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备