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Dorzolamide HCl

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Chemical Structure| 130693-82-2 同义名 : 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
CAS号 : 130693-82-2
货号 : A525496
分子式 : C10H17ClN2O4S3
纯度 : 98%
分子量 : 360.901
MDL号 : MFCD00884659
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：
生物活性
靶点

  • Carbonic Anhydrase IV

    Carbonic anhydrase IV, Ki:31 nM

  • Carbonic Anhydrase I

    Carbonic anhydrase I, Ki:6000 nM

  • Carbonic Anhydrase II

    Carbonic anhydrase II, Ki:1.9 nM
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].
实验方案
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
参考文献

[1]Josefsson A, Sigurdsson SB, et al. Dorzolamide induces vasodilatation in isolated pre-contracted bovine retinal arteries. Exp Eye Res. 2004 Feb;78(2):215-21.

[2]Gelatt KN, MacKay EO. Changes in intraocular pressure associated with topical dorzolamide and oral methazolamide in glaucomatous dogs. Vet Ophthalmol. 2001 Mar;4(1):61-7.

[3]Akin S, Ayaloglu H, Gultekin E, Colak A, Bekircan O, Akatin MY. Synthesis of 1,2,4-triazole-5-on derivatives and determination of carbonic anhydrase II isoenzyme inhibition effects. Bioorg Chem. 2019 Mar;83:170-179

[4]Sugrue MF. The preclinical pharmacology of dorzolamide hydrochloride, a topical carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1996 Fall;12(3):363-76

[5]Ali BM, Zaitone SA, Shouman SA, Moustafa YM. Dorzolamide synergizes the antitumor activity of mitomycin C against Ehrlich's carcinoma grown in mice: role of thioredoxin-interacting protein. Naunyn Schmiedebergs Arch Pharmacol. 2015 Dec;388(12):1271-82