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Dichlorphenamide/二氯苯二磺胺 {[allProObj[0].p_purity_real_show]}

货号:A201176 同义名: 双氯非那胺 / Diclofenamide

Dichlorphenamide是一种磺胺类化合物,也是口服生物利用度高的碳酸酐酶(CA)抑制剂,对人类 CAI、CAII、CAIX 和 CAXII 的 Ki 值分别为 1.20、38、50 和 50 nM。

Dichlorphenamide/二氯苯二磺胺 化学结构 CAS号:120-97-8
Dichlorphenamide/二氯苯二磺胺 化学结构
CAS号:120-97-8
Dichlorphenamide/二氯苯二磺胺 3D分子结构
CAS号:120-97-8
Dichlorphenamide/二氯苯二磺胺 化学结构 CAS号:120-97-8
Dichlorphenamide/二氯苯二磺胺 3D分子结构 CAS号:120-97-8
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Dichlorphenamide/二氯苯二磺胺 纯度/质量文件 产品仅供科研

货号:A201176 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Dichlorphenamide/二氯苯二磺胺 生物活性

靶点
  • Carbonic Anhydrase

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].

Dichlorphenamide/二氯苯二磺胺 临床研究

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 - -

Dichlorphenamide/二氯苯二磺胺 参考文献

[1]Kaup M, Plange N, et al. Effects of brinzolamide on ocular haemodynamics in healthy volunteers. Br J Ophthalmol. 2004 Feb;88(2):257-62.

[2]DeSantis L. Preclinical overview of brinzolamide. Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29.

[3]Kanski JJ. Carbonic anhydrase inhibitors and osmotic agents in glaucoma. Carbonic anhydrase inhibitors. Br J Ophthalmol. 1968 Aug;52(8):642-3

[4]Greig SL. Dichlorphenamide: A Review in Primary Periodic Paralyses. Drugs. 2016 Mar;76(4):501-7

[5]leckmann H. Die Wirkung von Dichlorphenamid bei der Behandlung des akuten Glaukomanfalls [Dichlorphenamide treatment in acute glaucoma (author's transl)]. Albrecht Von Graefes Arch Klin Exp Ophthalmol. 1976 Nov 18;201(1):69-77. German

Dichlorphenamide/二氯苯二磺胺 实验方案

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

Dichlorphenamide/二氯苯二磺胺 技术信息

CAS号120-97-8
分子式C6H6Cl2N2O4S2
分子量 305.16
SMILES Code O=S(C1=C(Cl)C(Cl)=CC(S(=O)(N)=O)=C1)(N)=O
MDL No. MFCD00148948
别名 双氯非那胺 ;Diclofenamide
运输蓝冰
InChI Key GJQPMPFPNINLKP-UHFFFAOYSA-N
Pubchem ID 3038
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方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;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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