产品
编 号：F718945
分子式：C9H11ClN2O4S
分子量：278.71
分子式：C9H11ClN2O4S
分子量：278.71
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CAS No: 871824-55-4
产品详情
生物活性：
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na+ channels and N-type Ca2+ channels, and is effective as a K+ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
体内研究：
JNJ-26489112 (i.p.) effectively blocks chemically-induced, forelimb clonic seizures in mice ( male CF-1 albino mice) that are caused by subcutaneous bicuculine (Bic), picrotoxin (Pic), or pentylenetetrazol (PTZ), with 1-h ED50 values of 197, 189, or 109 mg/kg, respectively.In adult male rats, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC (total exposure) values in plasma were 9090 ng/mL (33 μM), 53 min, 95%, 8.2 h, and 53,200 ng-h/mL. Linear, dose-related increases in exposure were observed at 10, 30, and 300 mg/kg. JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the Vdss is 390 mL/kg and the CL is 96 mL/h-kg. In female beagle dogs, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC values in plasma are 11,500 ng/mL (41 μM), 55 min, 83%, 20 h, and 212,000 ng-h/mL. . JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the the Vdss and CL values are 630 mL/kg and 30 mL/h-kg, respectively.
体外研究：
JNJ-26489112 inhibits calcium influx in response to depolarization (fluorescence-based assay) with an IC50 of 34 μM. In a whole-cell, patch-clamp experiment with low-frequency stimulation (0.07 Hz), intended to measure N-type channel activity directly, JNJ-26489112 causes a concentration-dependent increase in inhibition, with an IC50 of 70 μM. JNJ-26489112 is a KCNQ2 channel opener, particularly at -50 mV.
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na+ channels and N-type Ca2+ channels, and is effective as a K+ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
体内研究：
JNJ-26489112 (i.p.) effectively blocks chemically-induced, forelimb clonic seizures in mice ( male CF-1 albino mice) that are caused by subcutaneous bicuculine (Bic), picrotoxin (Pic), or pentylenetetrazol (PTZ), with 1-h ED50 values of 197, 189, or 109 mg/kg, respectively.In adult male rats, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC (total exposure) values in plasma were 9090 ng/mL (33 μM), 53 min, 95%, 8.2 h, and 53,200 ng-h/mL. Linear, dose-related increases in exposure were observed at 10, 30, and 300 mg/kg. JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the Vdss is 390 mL/kg and the CL is 96 mL/h-kg. In female beagle dogs, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC values in plasma are 11,500 ng/mL (41 μM), 55 min, 83%, 20 h, and 212,000 ng-h/mL. . JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the the Vdss and CL values are 630 mL/kg and 30 mL/h-kg, respectively.
体外研究：
JNJ-26489112 inhibits calcium influx in response to depolarization (fluorescence-based assay) with an IC50 of 34 μM. In a whole-cell, patch-clamp experiment with low-frequency stimulation (0.07 Hz), intended to measure N-type channel activity directly, JNJ-26489112 causes a concentration-dependent increase in inhibition, with an IC50 of 70 μM. JNJ-26489112 is a KCNQ2 channel opener, particularly at -50 mV.
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