产品
编 号：F041518
分子式：C20H25ClN2O
分子量：344.88
分子式：C20H25ClN2O
分子量：344.88
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
询价
询价
10mg
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50mg
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询价
结构图
CAS No: 1127498-03-6
产品详情
生物活性：
JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression.
体内研究：
JNJ-40411813 (ADX-71149) (5-20 mg/kg, 灌胃, 24 h 6次) 在 Glutamate (HY-N0455B) 的协同作用下，明显增强了大脑区域对谷氨酸反应，特别是皮质区、纹状体和海马。药代动力学分析RouteDose (mg/kg)AUCINF_obs (ng·h/mL)t1/2 (h)Tmax (h)Cmax (ng/mL)Clobs (L·h/kg)Vss_obs (L/kg)
i.v.2.51833±90///1.4±0.12.31.4±0.10.2
p.o.102250±4172.31±0.57938//
Animal Model:Male Wistar Rats (150 mg)
Dosage:5 mg/kg, 20 mg/kg
Administration:Oral Gavage (p.o.)
Result:Showed increasing in basal binding with an EC50 of 48 μM and a Combined with 10 μM glutamate, [35S]GTPγS binding with an EC50 of 7.3 μM and a maximal effect of 380%.
JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression.
体内研究：
JNJ-40411813 (ADX-71149) (5-20 mg/kg, 灌胃, 24 h 6次) 在 Glutamate (HY-N0455B) 的协同作用下，明显增强了大脑区域对谷氨酸反应，特别是皮质区、纹状体和海马。药代动力学分析RouteDose (mg/kg)AUCINF_obs (ng·h/mL)t1/2 (h)Tmax (h)Cmax (ng/mL)Clobs (L·h/kg)Vss_obs (L/kg)
i.v.2.51833±90///1.4±0.12.31.4±0.10.2
p.o.102250±4172.31±0.57938//
Animal Model:Male Wistar Rats (150 mg)
Dosage:5 mg/kg, 20 mg/kg
Administration:Oral Gavage (p.o.)
Result:Showed increasing in basal binding with an EC50 of 48 μM and a Combined with 10 μM glutamate, [35S]GTPγS binding with an EC50 of 7.3 μM and a maximal effect of 380%.
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