左乙拉西坦 T0192

Product Introduction
Bioactivity


英文名: Levetiracetam

描述: Levetiracetam (SIB-S1) 是一种化学增敏剂，增强 Temozolomide 对胶质母细胞瘤干细胞增殖和凋亡的影响。它调节 HDAC 水平，最终使 MGMT 沉默从而提高 Temozolomide 的有效性。它是一种抗癫痫药，可结合突触小泡蛋白 SV2A。

激酶实验: EDTA plasma (20 μL) is diluted with 30 μL of DPP-4 assay buffer (100 mM Tris and 100 mM NaCl, adjusted to pH 7.8 with HCl) and mixed with 50 μL of H-Ala-Pro-7-amido-4-trifluoromethylcoumarin. The 200 mM stock solution in dimethylformamide is diluted 1:1000 with water to yield a final concentration of 100 μM. The plate is incubated at room temperature for 10 min, and fluorescence in the wells is determined by using a Victor 1420 Multilabel Counter at an excitation wavelength of 405 nm and an emission wavelength of 535 nm. For the detection of DPP-4 activity in wound lysates, 100 μg of protein from the respective wound lysates are used instead of 20 μL of plasma. Active GLP-1 is also detected from 100 μg of respective wound tissue samples and analyzed by using the Mouse/Rat Total Active GLP-1 Assay Kit.

体外活性: 对完全杏仁核刺激的大鼠,即颞叶癫痫模型,Levetiracetam对病灶性和二次全身性发作表现出有效的抗痉挛活性.腹腔注射5.4 mg/kg到96 mg/kg Levetiracetam抑制声源性惊厥易感大鼠乱跑和强直阵挛性惊厥,这种作用具有剂量依赖性.腹腔注射13 mg/kg,27 mg/kg或54 mg/kg Levetiracetam,剂量依赖性抑制反复杏仁核刺激诱发的癫痫发作.17 mg/kg Levetiracetam对声音诱发的小鼠阵挛性惊厥产生有效的抑制作用.

体内活性: 在新鲜离体的大鼠CA1海马神经元中,Levetiracetam不可逆抑制平均大约18%的高电压激活的(HVA)钙离子电流。Levetiracetam选择性抑制CA1锥体海马神经元的N型Ca2+通道,逆转海马神经元中DMCM对GABA引起的电流的抑制作用。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (293.75 mM)
H2O : 17 mg/mL (100 mM)


关键字: DNMTs | chemosensitizer | vesicle | inhibit | antiepileptic | Temozolomide | DNA Methyltransferase | HDA | Inhibitor | Levetiracetam | SV2A | UCB L-059 | synaptic | protein | DNA MTases | MGMT | UCB L 059 | glioblastoma | apoptosis

相关产品: CM-579 | Cedazuridine | Nanaomycin A | TFMB-(S)-2-HG | Hinokitiol | γ-Oryzanol | GSK3685032 | SW155246 | Tetrahydrouridine | DC-05

相关库: Drug Repurposing Compound Library | Anti-Hypertension Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途