Dorzolamide
Dorzolamide Basic information
- Product Name:
- Dorzolamide
- Synonyms:
-
- DORZOLAMIDE
- DORZOLAMIDE(SUBJECTTOPATENTFREE)
- 4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4S,6S)-
- 4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, (4S-trans)-
- 4S,6S-Dorzolamide
- (4S,6S)-4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide
- (4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-7,
- Dorzalamide hydrochloride
- CAS:
- 120279-96-1
- MF:
- C10H16N2O4S3
- MW:
- 324.44
- EINECS:
- 1533716-785-6
- Mol File:
- 120279-96-1.mol
Dorzolamide Chemical Properties
- Boiling point:
- 575.8±60.0 °C(Predicted)
- Density
- 1.53±0.1 g/cm3(Predicted)
- storage temp.
- room temp
- solubility
- DMSO: soluble5mg/mL (clear solution, warmed)
- pka
- pKa 6.35 (Uncertain);8.50 (Uncertain)
- form
- powder
- color
- white to beige
- optical activity
- [α]/D -25 to -35°, c = 1 in methanol
- CAS DataBase Reference
- 120279-96-1(CAS DataBase Reference)
Dorzolamide Usage And Synthesis
Uses
Carbonic anhydrase inhibitor.
Uses
Dorzolamide is an intermediate in synthesizing N-Acetyl Dorzolamide (A173640), a useful synthetic compound.
Definition
ChEBI: 5,6-Dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide in which hydrogens at the 4 and 6 positions are substituted by ethylamino and methyl groups, respectively (4S, trans-configuration . A carbonic anhydrase inhibitor, it is used as the hydrochloride in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension.
brand name
Trusopt (Merck).
Biological Activity
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.
in vivo
Dorzolamide (3, 10, or 30 mg/kg/day, ip) synergized mitomycin C exhibits anti-tumor activity in EAC solid tumor models. Dorzolamide produces a dose-dependent decrease in the calculated ratio (relative value of 57.3±1, 25.5±1.8, and 24.3± 0.7 %, respectively)[3].
| Animal Model: | Female Swiss albino mice (EAC solid tumor)[3]. |
| Dosage: | 3, 10, or 30 mg/kg/day (synergized mitomycin C). |
| Administration: | IP, daily for 3 weeks. |
| Result: | Upregulated TXNIP and p53 while downregulated bcl-2. Effective in retarding the growth of EAC in mice. |
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Dorzolamide(120279-96-1)Related Product Information
- Dorzolamide Hydrochloride
- METSULFURON METHYL
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- Acrylamide
- Erucamide
- Boc-D-Glutamine
- Nicotinamide
- 1,4-Dioxane
- Polyamide
- Methyl salicylate
- Selenium dioxide
- Tribenuron methyl
- Ceramide
- N,N-Dimethylformamide
- Kresoxim-methyl
- Polyacrylamide
- Thiophanate-methyl
- (4S)-4-Acetamide-5,6-Dihydro-6-Methyl-2-Sulfonamide-Thio[2,3-B]Thiopyran7,7Dioxide