Product Data?SheetTopiramateCat. No.:CAS No.:分?式:分?量:作?靶点:HY-B012297240-79-4C??H??NO?S339.36iGluR; GABA Receptor; Sodium Channel; Calcium Channel; Potassium Channel; Carbonic Anhydrase作?通路:Membrane Transporter/Ion Channel; Neuronal Signaling; Metabolic Enzyme/Protease储存?式:PowderIn solvent-20°C4°C-80°C-20°C3 years2 years6 months1 monthInhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : ≥ 100 mg/mL (294.67 mM)H2O : 4 mg/mL (11.79 mM; Need ultrasonic)* \Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM2.9467 mL0.5893 mL0.2947 mL14.7336 mL2.9467 mL1.4734 mL29.4672 mL5.8934 mL2.9467 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；?旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存?式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?式配制澄清的储备液，再依次添加助溶剂： 为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。Page 1 of 2 www.MedChemExpress.cn
2. 请依序添加每种溶剂：?10% DMSO ?? 90% (20% SBE-β-CD in saline)Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
此?案可获得 ≥ 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液。
以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合均匀。
3. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilSolubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution
此?案可获得 ≥ 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。
BIOLOGICAL ACTIVITY
?物活性
Topiramate (McN 4853) 是?种?谱抗癫痫药。Topiramate 也是?种 GluR5 受体拮抗剂，可通过增强 GABAergic 活性，抑制 kainate/AMPA 受体，抑制钠和钙通道的电压敏感，增加钾电导并抑制 carbonic anhydrase 来产?抗癫痫作?。
IC?? & Target
GluR5 receptor[1]; GABAergic[2]; Kainate/AMPA[2]; Sodium channel[2]; Calcium channel[2]; Potassium channel[2]; Carbonic anhydrase[2]
体外研究
Topiramate has been believed to be a type of antiepileptic drug that blocks spread of seizures. Thus far, the
mechanisms of its actions have been proven to include use-dependent inhibition of voltage-dependent Na+ channels in neurons, potentiation of GABA (γ-amino-butyric acid)-induced Cl- influx, and inhibitory effects on inward currents by antagonizing kainate/alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors[2].
客户使?本产品发表的科研?献
????Personalized Medicine Universe.?2019 May.?
See more customer validations on www.MedChemExpress.cnREFERENCES
[1].?Lyseng-Williamson KA, et al. Topiramate: a review of its use in the treatment of epilepsy. Drugs. 2007;67(15):2231-56.
[2].?Nakamura J, et al. Target pharmacology of topiramate, a new antiepileptic drug. Nihon Yakurigaku Zasshi. 2000 Jan;115(1):53-7.
[3].?Kaminski RM, et al. Topiramate selectively protects against seizures induced by ATPA, a GluR5 kainate receptor agonist. Neuropharmacology. 2004 Jun;46(8):1097-104.
McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.
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