hCAI/II-IN-6 是一种具有口服活性的human Carbonic Anhydrase(CA) 抑制剂。hCAI/II-IN-6 选择性地抑制 hCA II 和 hCA VII,对 hCA I,hCA II,hCA VII 和 hCA XII 的Ki值分别为 220,4.9,6.5 和 >50000 nM。hCAI/II-IN-6 在体内显示抗惊厥活性和抗最大电击 (MES) 活性。hCAI/II-IN-6 可以用于癫痫的研究。
产品描述
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with K i 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].
体外活性
hCAI/II-IN-6 (0-50 μM) inhibits hCA I, hCA II, hCA VII and hCA XII activities with K i values of 220, 4.9, 6.5 and >50000 nM, respectively [1].
体内活性
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 ED 50 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.
Cas No.
694466-00-7
分子式
C19H24N4O3S
分子量
388.48
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years