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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Dorzolamide (L671152; MK507; L671152; MK507; Trusopt) is a CAI (carbonic anhydrase inhibitors) approved for use as an anti-glaucoma agent. It is a water-soluble and potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively.
ln Vitro |
Dorzolamide blocks Component A, which is generated by CO2 influx and hydration by CA-II, in a dose-dependent manner with an IC50 of 2.4 μM (95% confidence interval: 0.5-10.85 μM) for 50% inhibitory concentration [2].
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ln Vivo |
In an EAC solid tumor model, dorzolamide (3, 10, or 30 mg/kg/day, intraperitoneally) has anticancer efficacy when combined with mitomycin C. The computed ratios (relative values 57.3±1, 25.5±1.8, and 24.3±0.7%, respectively) decline with dorzolamide dosage [3].
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Animal Protocol |
Animal/Disease Models: Female Swiss albino mouse (EAC solid tumor) [3].
Doses: 3, 10 or 30 mg/kg/day (with mitomycin C). Doses: IP, one time/day for 3 weeks. Experimental Results: TXNIP and p53 were up-regulated, and bcl-2 was down-regulated. Effectively delays 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
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Molecular Weight |
324.44
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Exact Mass |
324.0272
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CAS # |
120279-96-1
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Related CAS # |
Dorzolamide hydrochloride;130693-82-2;Dorzolamide-d5;1227097-70-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=S(C(S1)=CC2=C1S([C@@H](C)C[C@@H]2NCC)(=O)=O)(N)=O
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Synonyms |
L671152MK507 L671152 MK507 Trusopt UNII-9JDX055TW1 UNII9JDX055TW1 UNII 9JDX055TW1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0822 mL | 15.4112 mL | 30.8223 mL | |
5 mM | 0.6164 mL | 3.0822 mL | 6.1645 mL | |
10 mM | 0.3082 mL | 1.5411 mL | 3.0822 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.