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Purity: ≥98%
Dorzolamide HCl (also known as MK-507; L-671152 HCl; L671152; MK507; trade name Trusopt), an anti-glaucoma agent and CAI (carbonic anhydrase inhibitors), is a water-soluble and potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively. Dorzolamide wa approved for use as an anti-glaucoma agent that is topically applied in the form of eye drops. Dorzolamide hydrochloride is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.
| ln Vitro |
Dorzolamide hydrochloride inhibits Component A, which is brought on by the CO2 inflow and the hydration of CA-II that follows, in a dose-dependent manner with an IC50 of 2.4 μM [2].
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| ln Vivo |
In an EAC solid tumor model, dorzolamide hydrochloride (3, 10, or 30 mg/kg/day, i.p.) has anticancer efficacy in conjunction with mitomycin C. The calculated ratios (relative values 57.3±1, 25.5±1.8, and 24.3±0.7%, respectively) were dose-dependently lowered by dorzolamide hydrochloride [3].
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| Animal Protocol |
Animal/Disease Models: Female Swiss albino mice (EAC solid tumor)[3].
Doses: 3, 10, or 30 mg/kg/day (synergized mitomycin C). Route of Administration: IP, daily for 3 weeks. Experimental Results: Upregulated TXNIP and p53 while downregulated bcl-2. Effective in retarding the growth of EAC in mice. |
| References |
[1]. J Biollaz, et al. Whole-blood pharmacokinetics and metabolic effects of the topical carbonic anhydrase inhibitor dorzolamide. Eur J Clin Pharmacol. 1995;47(5):455-60.
[2]. Sangly P Srinivas, et al. Inhibition of carbonic anhydrase activity in cultured bovine corneal endothelial cells by dorzolamide. Invest Ophthalmol Vis Sci. 2002 Oct;43(10):3273-8. [3]. Belal M Ali, et al. 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. |
| Molecular Formula |
C10H16N2O4S3.HCL
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| Molecular Weight |
360.9
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| CAS # |
130693-82-2
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| Related CAS # |
Dorzolamide;120279-96-1
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| SMILES |
O=S(C(S1)=CC2=C1S([C@@H](C)C[C@@H]2NCC)(=O)=O)(N)=O.Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7709 mL | 13.8543 mL | 27.7085 mL | |
| 5 mM | 0.5542 mL | 2.7709 mL | 5.5417 mL | |
| 10 mM | 0.2771 mL | 1.3854 mL | 2.7709 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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