Sultiame is an inhibitor of carbonic anhydrase that used to treat epilepsy.
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产品名称 | Carbonic Anhydrase ↓ ↑ | Carbonic Anhydrase I ↓ ↑ | Carbonic Anhydrase II ↓ ↑ | Carbonic Anhydrase IV ↓ ↑ | Carbonic Anhydrase IX ↓ ↑ | Carbonic Anhydrase XII ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Topiramate | ✔ | Calcium Channel | 98% | ||||||||||||||||
Dichlorphenamide | ✔ | 98% | |||||||||||||||||
Mafenide Acetate | ✔ | 98% | |||||||||||||||||
Benzenesulphonamide | ✔ | 98% | |||||||||||||||||
Dorzolamide HCl |
+
Carbonic anhydrase I, Ki: 6000 nM |
++++
Carbonic anhydrase II, Ki: 1.9 nM |
+++
Carbonic anhydrase IV, Ki: 31 nM |
98% | |||||||||||||||
Methazolamide |
++
hCAI, Ki: 50 nM |
+++
hCAII, Ki: 14 nM |
++
bCAIV, Ki: 36 nM |
98% | |||||||||||||||
Tioxolone |
+
CAI, Ki: 91 nM |
98% | |||||||||||||||||
U-104 |
++
CAIX, Ki: 45.1 nM |
++++
CAXII, Ki: 4.5 nM |
98% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Sultiame is a carbonic anhydrase (CA) inhibitor, widely used as an antiepileptic drug[2]. CA inhibitors (CAIs) such as acetazolamide, methazolamide, topiramate, zonisamide, and sulthiame (Sultiame) can reduce seizures through perturbation of the CO(2) equilibrium and/or the inhibition of ion channels[3]. Drugs inhibiting metabolism include antibiotic macrolides, chloramphenicol, isoniazide, some sulphonamides, propoxyphene, cimetidine, valproic acid and sulthiame. Anti-epileptic drugs can induce hepatic microsomal enzymes and, therefore, may increase metabolism of corticosteroids, oral contraceptives, oral anticoagulants, cardiovascular agents, antibiotics, chemotherapeutic agents, psychotropic drugs and non-opiate analgesics, thereby reducing their efficacy[4]. The high tolerability, efficacy, convenience of use and low cost suggest that sulthiame should become a first line drug in the benign partial epilepsies of childhood and juvenile myoclonic epilepsy. It also has a role as add-on treatment in other partial and myoclonic epilepsies[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03400189 | Epilepsy | Phase 1 | Active, not recruiting | August 30, 2018 | Switzerland ... 展开 >> Division of Clinical Pharmacology Lausanne, Vaud, Switzerland, 1011 收起 << |
NCT00471744 | Epilepsy, Rolandic | Phase 3 | Terminated(low patient number ... 展开 >>after 2 years recruiting) 收起 << | - | Germany ... 展开 >> Dr. von Haunersches Kinderspital München, Germany, 81371 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.44mL 0.69mL 0.34mL |
17.22mL 3.44mL 1.72mL |
34.44mL 6.89mL 3.44mL |
CAS号 | 61-56-3 |
分子式 | C10H14N2O4S2 |
分子量 | 290.359 |
别名 | Sulthiame |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(172.2 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |