1. Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. Calcium Channel
    Sodium Channel
    Potassium Channel
  3. JNJ-26489112

JNJ-26489112 

Cat. No.: HY-12596
Handling Instructions

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).

For research use only. We do not sell to patients.

JNJ-26489112 Chemical Structure

JNJ-26489112 Chemical Structure

CAS No. : 871824-55-4

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Description

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)[1].

In Vitro

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[1].

In Vivo

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[1].
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[1].

Molecular Weight

278.71

Formula

C₉H₁₁ClN₂O₄S

CAS No.

871824-55-4

SMILES

O=S(N)(NC[[email protected]@H]1OC2=CC=C(Cl)C=C2OC1)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

JNJ-26489112JNJ26489112JNJ 26489112Calcium ChannelSodium ChannelPotassium ChannelCa2+ channelsCa channelsNa channelsNa+ channelsKcsAbroad-spectrumanticonvulsantseizuresfrequencystimulationsulfamidederivativesInhibitorinhibitorinhibit

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