hCAI/II-IN-6

hCAI/II-IN-6 is a human carbonic anhydrase(CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase

Research Areas >> Neurological Disease

hCAI/II-IN-6 (0-50 μM) inhibits hCA I, hCA II , hCA VII and hCA XII activities with Ki values of 220, 4.9, 6.5 and ＞50000 nM, respectively[1].

hCAI/II-IN-6 (30-100mg/kg; i.p. once) shows good anticonvulsant effect in vivo[1]. hCAI/II-IN-6 (30 mg/kg; p.o. once) shows anti-MES activity in vivo[1]. Animal Model: Swiss albino mice[1] Dosage: 30 and 100 mg/kg Administration: Intraperitoneal injection; 30-100 mg/kg once Result: Provided seizure attenuation and good anticonvulsant effect, and showed an ED50 of 13.7mg/kg in anticonvulsant quantification study. Animal Model: Wistar albino rats[1] Dosage: 30 mg/kg Administration: Oral gavage; 30 mg/kg once Result: Showed anti-MES activity and significant protection from seizures up to 1h of drug administration and action was gone reduced after 1h.

[1]. Mishra CB, et al. Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. J Med Chem. 2017 Mar 23;60(6):2456-2469.