Zonisamide (AD 810) sodium 是一种口服有效的碳酸酐酶 (carbonic anhydrase) 抑制剂，对人类线粒体同工酶hCA II和hCA V的Ki值分别为 35.2 nM 和 20.6 nM。Zonisamide sodium 可通过抗细胞凋亡和上调MnSOD水平来发挥神经保护作用。Zonisamide sodium 还能增加Hrd1的表达，从而改善 AAC 大鼠的心脏功能。Zonisamide sodium 可用于癫痫、帕金森和心脏肥大的研究。
| 生物活性 | Zonisamide (AD 810) sodium is an orally activecarbonic anhydraseinhibitor, withKis of 35.2 and 20.6 nM forhCA IIandhCA V, respectively. Zonisamide sodium exerts neuroprotective effects through anti-apoptosisand upregulatingMnSODlevels. Zonisamide sodium also increases the expression ofHrd1, thereby improving cardiac function in AAC rats. Zonisamide sodium can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy[1][2][3][4]. |
| IC50& Target | Ki: 35.2μM (hCA II) , 20.6 nM (hCA V)[2] |
体外研究
(In Vitro) | Zonisamide sodium (10, 50, 100, 200 μM; 24 h) increases viability of SH-SY5Y cells via an anti-apoptotic effect[1].
Zonisamide sodium (100 μM; 24 h) shows neuroprotective effects in PD-cellular models. (PD: parkinson’s disease)[1].
Zonisamide sodium (100 μM; 24 h) reduces levels of proapoptotic molecules, and upregulates levels of MnSOD (MnSOD over-expression attenuates MPTP toxicity and protects cells from apoptosis)[1].
Zonisamide sodium (0.1, 0.3, 1 μM; 24 h) inhibits cardiac hypertrophy and fibrosis in vitro[3].
Zonisamide sodium markedly increases the expression of Hrd1 in Ang II-treated NRCMs[3].
Cell Viability Assay[1] | Cell Line: | SH-SY5Y cells | | Concentration: | 10, 50, 100, 200 μM | | Incubation Time: | 24 h | | Result: | Induced an increase of cell viability, and with the greatest effect being at 100 μM.
Exhibited neuroprotective effect on SH-SY5Y cells (PD-cellular models) when at 100 μM. |
Apoptosis Analysis[1] | Cell Line: | SH-SY5Y cells | | Concentration: | 100 μM | | Incubation Time: | 24 h | | Result: | Showed an effect of anti-apoptotic. |
RT-PCR[3] | Cell Line: | NRCMs and cardiac fibroblasts (expose to Ang II for cardiomyocyte hypertrophy and fibrosis model) | | Concentration: | 0.1, 0.3, 1 μM | | Incubation Time: | 24 h | | Result: | Decreased the expression of atrial natriuretic factor (ANF) and cardiomyosin heavy chain β (β-MHC) but increased the expression of cardiac myosin heavy chain α (α-MHC) in NRCMs.
Decreased cardiac expression of the fibrosis-related gene Collagen 1A1 (Col1A1) in cardiac fibroblasts. |
Western Blot Analysis[1] | Cell Line: | SH-SY5Y cells | | Concentration: | 100 μM | | Incubation Time: | 24 h | | Result: | Reduced the proapoptotic molecules levels of cleaved caspase-9, -3, and p-JNK, and blocked the activation of proapoptotic molecules in SH-SY5Y cells.
Induced an increase in MnSOD levels.(MnSOD over-expression attenuates MPTP toxicity and protects cells from apoptosis). |
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体内研究
(In Vivo) | Zonisamide sodium (40 mg/kg; i.p.; single daily for 14 days) prevents seizures in FeCl3-induced chronic amygdalar seizures model[2].
Zonisamide sodium (14, 28, 56 mg/kg; i.p.; single daily for 6 weeks) alleviates cardiac hypertrophy and improved cardiac function in rats subjected to AAC (abdominal aortic constriction)[3].
Zonisamide sodium (14, 28, 56 mg/kg; i.p.; single daily for 6 weeks) upregulates Hrd1 expression and accelerates ERAD in the hearts of AAC rats[3].
| Animal Model: | Male Wistar rats (200-250 g; FeCl3-induced chronic amygdalar seizures)[2]. | | Dosage: | 40 mg/kg | | Administration: | Intraperitoneal injection; single daily for 14 days. | | Result: | Showed activity of anti-seizures.
Significantly down-regulated GABA transporters GAT-1 in the hippocampus. |
| Animal Model: | Adult male Sprague-Dawley rats (100-120 g; cardiac hypertrophy model)[3]. | | Dosage: | 14, 28, 56 mg/kg (dissolved in 1% DMSO) | | Administration: | Intraperitoneal injection; single daily for 6 weeks. | | Result: | Significantly attenuated cardiac hypertrophy and fibrosis.
Increased LV ejection fraction (EF), fractional shortening (FS) and E/A ratio.
Markedly increased the expression of Hrd1 in the hearts of AAC rats. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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