Dorzolamide is a potent carbonic anhydrase II inhibitor with an IC50 value of 0.16 nM on human erythrocyte carbonic anhydrase II in vitro. It has been found to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.
| Molecular Weight | 324.44 |
| Formula | C10H16N2O4S3 |
| CAS Number | 120279-96-1 |
| Solubility (25°C) | DMSO: 5 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Thorsteinn Loftsson, et al. Topical drug delivery to the eye: dorzolamide
[3] Jens Martens-Lobenhoffer, et al. Clinical pharmacokinetics of dorzolamide
| Related Carbonic Anhydrase Products |
|---|
| Acetazolamide sodium
Acetazolamide sodium is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX.Acetazolamide reduces the production of intraocular aqueous humor and may be used in glaucoma-related studies. |
| WES-1
WES-1 is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). |
| CA inhibitor 2
CA inhibitor 2 is a carbonic anhydrase inhibitor (IC50: 0.033 μM). |
| hCA XII-IN-6
hCA XII-IN-6 is a potent hCA XII inhibitor with a Ki value of 84.2 nM. |
| Carbonic anhydrase inhibitor 15
Carbonic anhydrase inhibitor 15 is a carbonic anhydrase inhibitor (Ki: 8.5 nM for hCA II). |
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