货号:A525496 同义名: MK-507;L-671,152
Dorzolomide HCl is a potent and water-soluble inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM respectively and used as anti-glaucoma agent.
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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 |
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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 | Carbonic anhydrase (CA) II, a physiologically predominant isoform in CA enzymes, is found in red blood cells and many other tissues and plays major roles in pH regulation of body, protection of electrolyte balance, transportation of water and some metabolic pathways[3]. Dorzolamide hydrochloride, approved in patients with ocular hypertension or open-angle glaucoma, is a water-soluble, potent inhibitor of human CA II and CA IV in vitro, the respective IC50 values being 0.18 nM and 6.9 nM. In contrast, it was found to be a much weaker inhibitor of human CA I (IC50 value of 600 nM). In vivo, the topical administration of one 50 microliters drop of 0.5%, 1% and 2% solutions of dorzolamide maximally lowered the intraocular pressure (IOP) of glaucomatous monkeys by 22%, 30% and 37%, respectively. Good ocular hypotensive activity was also observed in ocular normotensive and hypertensive rabbits[4]. Moreover, dorzolamide (3, 10, or 30 mg/kg/day, ip) synergized the antitumor activity of mitomycin C in EAC (Ehrlich's ascites carcinoma) solid tumor models[5]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.85mL 2.77mL 1.39mL |
27.71mL 5.54mL 2.77mL |
CAS号 | 130693-82-2 |
分子式 | C10H17ClN2O4S3 |
分子量 | 360.901 |
别名 | MK-507;L-671,152;(4Strans)4(ethylamino)56dihydro6methyl4Hthieno23bthiopyran2sulfonamide 77dioxide monohydrochloride.;(2S4S)2Ethylamino4methyl55dioxo57dithiabicyclo4.3.0nona810diene8sulfonamide hydrochloride;TRUSOPT;Dorzolamide (hydrochloride);MK-507 HCl;MK507 hydrochloride;L671152 hydrochloride;Dorzolamide hydrochloride |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(290.94 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 H2O: 12 mg/mL(33.25 mM),配合低频超声助溶 |
动物实验配方 |