| Description |
hCAI/II-IN-4 (compound 6d) is a potent dual hCA I/II inhibitor with Ki values of 16.95, 15.22 and 27.04 nM for hCA I, hCA II and hCA Ⅸ, respectively. hCAI/II-IN-4 has anti-hypoxia activities and low toxicity. hCAI/II-IN-4 can be used for acute mountain sickness (AMS) research[1].
|
| Related Catalog |
|
| Target |
Ki:16.95 nM (hCA I)、15.22 nM (hCA II) and 27.04 nM (hCA Ⅸ)
|
| In Vitro |
hCAI/II-IN-4 (compound 6d) (5-200μM; 48 hours) has no apparent cytotoxicity in HEK293 cells[1]. Cell Cytotoxicity Assay[1] Cell Line: HEK293 cells Concentration: 5, 25, 50, 100 and 200 μM Incubation Time: 48 hours Result: The cell viability rate was higher than 60%.
|
| In Vivo |
hCAI/II-IN-4 (compound 6d) (400-2000 mg/kg; p.o.; Male BLAB/c mice of hypoxia) has no apparent toxic effect in vivo[1]. Animal Model: Male BLAB/c mice of hypoxia[1] Dosage: 400, 500 and 2000 mg/kg Administration: Oral administration Result: Prolonged the survival time of mice by 29.3% compared with that of the blank control group.
|
| References |
[1]. Yang C, et al. N-Quinary heterocycle-4-sulphamoylbenzamides exert anti-hypoxic effects as dual inhibitors of carbonic anhydrases I/II. Bioorg Chem. 2020 Jul;100:103931.
|
