| Description | hCAI/II-IN-6 is a selective and orally active inhibitor of human carbonic anhydrase (CA). hCAI/II-IN-6 inhibited hCA I, hCA II, hCA VII, and hCA XII with Ki values of 220, 4.9, 6.5, and ＞50,000 nM. hCAI/II-IN-6 showed anticonvulsant activity in vivo. hCAI/II-IN-6 can be used to study epilepsy. hCAI/II-IN-6 showed anticonvulsant activity in vivo. hCAI/II-IN-6 can be used to study epilepsy. |
| In vitro | hCAI/II-IN-6 (0-50 μM) 对 hCA I、hCA II、hCA VII 和 hCA XII 的活性表现出抑制效果，其 Ki 值分别为 220 nM、4.9 nM、6.5 nM 和 >50000 nM。[1] |
| In vivo | In vivo, hCAI/II-IN-6 (30-100mg/kg; i.p. once; Swiss albino mice) provided seizure attenuation and good anticonvulsant effect and showed an ED 50 of 13.7mg/kg in anticonvulsant quantification study. [1] In vivo, hCAI/II-IN-6 (30 mg/kg; p.o.; once; Swiss albino mice) has been observed to possess anti-MES (maximal electroshock seizure) activity.[1] |
| Target activity | CA XII (human):＞50000 nM(Ki ), CA VII (human):6.5 nM(Ki ), CA (human):220 nM(Ki ), CA II (human):4.9 nM(Ki ) |
| molecular weight | 388.48 |
| Molecular formula | C19H24N4O3S |
| CAS | 694466-00-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 225.0 mg/mL (579.2 mM), Sonication is recommended. |
| References | 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;60(6):2456-2469. |