货号:A201176 同义名: 双氯非那胺 / Diclofenamide
Dichlorphenamide is a sulfonamide and an orally bioavailable carbonic anhydrase (CA) inhibitor with Kis of 1.20, 38, 50, and 50 nM for the human CA isoforms CAI, CAII, CAIX, and CAXII, respectively.
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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 | |||||||||||
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Topiramate | ✔ | Calcium Channel | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Dichlorphenamide | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mafenide Acetate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Benzenesulphonamide | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Dorzolamide HCl |
+
Carbonic anhydrase I, Ki: 6000 nM |
++++
Carbonic anhydrase II, Ki: 1.9 nM |
+++
Carbonic anhydrase IV, Ki: 31 nM |
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Methazolamide |
++
hCAI, Ki: 50 nM |
+++
hCAII, Ki: 14 nM |
++
bCAIV, Ki: 36 nM |
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Tioxolone |
+
CAI, Ki: 91 nM |
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U-104 |
++
CAIX, Ki: 45.1 nM |
++++
CAXII, Ki: 4.5 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
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。 |
靶点 |
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描述 | Dichlorphenamide is a carbonic anhydrase inhibitor that is used in the treatment of glaucoma. This drug has the same side-effects as acetazolamide, for which it is a useful substitute, except for a lesser tendency to cause dermatitis, renal calculi and metabolic acidosis. It may induce a more pronounced renal loss of potassium[3]. In two trials in patients with hypokalaemic periodic paralysis, dichlorphenamide was associated with a significantly (eightfold) lower paralytic attack rate and fewer patients with acute intolerable worsening compared with placebo. Dichlorphenamide is a valuable treatment option for patients with primary hyperkalaemic or hypokalaemic periodic paralysis[4]. Dichlorphenamide as well as Diamox lowers intraocular pressure. For adequate treatment of acute glaucoma only 20% of commonly used Diamoxdosis is requested to reach comparable pressure release two hours later. After one hour control intraocular pressure of 60% from patients with Dichlorphenamide treatment was found below 40 mm Hg since in Diamoxgroup there were only 30% below 40 mm Hg. Essential side effects after a single dosis of 200 mg Dichlorphenamide or in combination with Diamox for acute glaucoma treatment could not be observed[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00494507 | Hyperkalemic Periodic Paralysi... 展开 >>s Hypokalemic Periodic Paralysis 收起 << | Phase 3 | Completed | - | United States, California ... 展开 >> UCLA Neurology Los Angeles, California, United States, 90095 University of California-San Francisco San Francisco, California, United States, 94143 United States, Kansas University of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, Massachusetts Brigham & Women's Hospital Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, New York Columbia University Medical Center New York, New York, United States, 10032 University of Rochester Rochester, New York, United States, 14642 United States, Ohio Ohio State University Columbus, Ohio, United States, 43210 United States, Texas University of Texas Southwestern-Dallas Dallas, Texas, United States, 75390 Italy University of Milan San Donato, Milan, Italy United Kingdom Institute of Neurology-Queen's Square London, United Kingdom 收起 << |
NCT00004802 | Paralysis, Hyperkalemic Period... 展开 >>ic Hypokalemic Periodic Paralysis Paramyotonia Congenita 收起 << | Phase 3 | Completed | - | - |
NCT00494507 | - | Completed | - | - |
[2]DeSantis L. Preclinical overview of brinzolamide. Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29.
[4]Greig SL. Dichlorphenamide: A Review in Primary Periodic Paralyses. Drugs. 2016 Mar;76(4):501-7
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.28mL 0.66mL 0.33mL |
16.38mL 3.28mL 1.64mL |
32.77mL 6.55mL 3.28mL |
CAS号 | 120-97-8 |
分子式 | C6H6Cl2N2O4S2 |
分子量 | 305.159 |
别名 | 双氯非那胺 ;Diclofenamide |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(344.08 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 |