hCAI/II-IN-6

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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 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.

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.

hCAI/II-IN-6 (30-100mg/kg; i.p. once) shows good anticonvulsant effect in vivo.hCAI/II-IN-6 (30 mg/kg; p.o. once) shows anti-MES activity in vivo.Animal Model:Swiss albino miceDosage: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 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.

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Membrane Transporter/Ion Channel

Carbonic Anhydrase

Carbonic Anhydrase

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694466-00-7

388.48

C19H24N4O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (643.53 mM; 超声助溶 )

NS(=O)(=O)c1ccc(NC(=O)CN2CCN(Cc3ccccc3)CC2)cc1

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(-20℃)

With Ice Pack

≥ 2 years