Dorzolamide HCl

Dorzolamide HCl

Product Code: 3121
Availability: In Stock
$133.00
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Dorzolamide HCl is a carbonic anhydrase inhibitor.

Chemical Name:

4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, hydrochloride

Biological Activity:
Biological Activity Dorzolamide HCL is a hydrochloride salt of dorzolamide. Dorzolamide is a potent inhibitor of human carbonic anhydrase isoenzyme II. The IC50 of dorzolamide is 0.18 nM in vitro. For a comparison, the inhibitory activity of dorzolamide against human carbonic anhydrase isozyme I is much weaker with an IC50 of 600 nM.[1] When 20 or 200 µM dorzolamide is incubated with human erythrocytes, 98% or 71% of dorzolamide is taken up by the erythrocytes, respectively. Dorzolamide has a high affinity for human carbonic anhydrase isoenzyme II with a Kd of 1.1 nM. [2] Dorzolamide decreases intraocular pressure via reducing aqueous humor production
Technical Data:
M.W. 360.9
Formula: C<sub>10</sub>H<sub>16</sub>N<sub>2</sub>O<sub>4</sub>S<sub>3</sub>.HCl
Solubility: DMSO
Purity: 98%
Storage: -20℃
CAS No: 130693-82-2
References:
References Plummer CE, MacKay EO, Gelatt KN: Comparison of the effects of topical administration of a fixed combination of dorzolamide-timolol to monotherapy with timolol or dorzolamide on IOP, pupil size, and heart rate in glaucomatous dogs. Vet Ophthalmol. 2006 Jul-Aug;9(4):245-9. Grover S, Apushkin MA, Fishman GA: Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosa. Am J Ophthalmol. 2006 May;141(5):850-8. Epub 2006 Mar 20. Almeida GC Jr, Faria e Souza SJ: Effect of topical dorzolamide on rabbit central corneal thickness. Braz J Med Biol Res. 2006 Feb;39(2):277-81. Epub 2006 Feb 2. Martens-Lobenhoffer J, Banditt P: Clinical pharmacokinetics of dorzolamide. Clin Pharmacokinet. 2002;41(3):197-205 Balfour JA, Wilde MI: Dorzolamide. A review of its pharmacology and therapeutic potential in the management of glaucoma and ocular hypertension. Drugs Aging. 1997 May;10(5):384-403. Ponticello GS, Sugrue MF, Plazonnet B, Durand-Cavagna G: Dorzolamide, a 40-year wait. From an oral to a topical carbonic anhydrase inhibitor for the treatment of glaucoma. Pharm Biotechnol. 1998;11:555-74.

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