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JNJ-26489112 

Cat. No. M30775
JNJ-26489112  Structure
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Biological Activity

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).

Chemical Information
Molecular Weight 278.71
Formula C9H11ClN2O4S
CAS Number 871824-55-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Dirk Mariën, et al. Reprod Toxicol. Timing is everything for sperm assessment in fertility studies

[2] Gaetano Zaccara, et al. Pharmacol Res. Do traditional anti-seizure drugs have a future? A review of potential anti-seizure drugs in clinical development

[3] G Eichenbaum, et al. Regul Toxicol Pharmacol. Implications of retinal effects observed in chronic toxicity studies on the clinical development of a CNS-active drug candidate

[4] Nicholas A Di Prospero, et al. Epilepsy Res. Evaluation of JNJ-26489112 in patients with photosensitive epilepsy: a placebo-controlled, exploratory study

[5] David F McComsey, et al. J Med Chem. Novel, broad-spectrum anticonvulsants containing a sulfamide group: pharmacological properties of (S)-N-[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112)

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  Catalog
Abmole Inhibitor Catalog




Keywords: JNJ-26489112  supplier, Calcium Channel, inhibitors, activators


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