Dorzolamide HCL Inhibitor CAS No. 130693-82-2

Cat. No.	Name	Size	Price
KI1284	Dorzolamide HCL	10 mg	$176
	Dorzolamide HCL	25 mg	$272
	Dorzolamide HCL	100 mg	$752

Chemical Characteristic

Product Name	Dorzolamide HCL
Synonyms	Trusopt, L-671152, MK-507
CAS No.	130693-82-2
Molecular Weight	360.89
Formula	C₁₀H₁₇ClN₂O₄S₃
Smiles	[C@@H]1(C[C@@H](c2c(S1(=O)=O)sc(c2)S(=O)(=O)N)NCC)C Cl
Chemical Structure

Biological activities

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.^[3]

Protocols

In vitro: Dorzolamide is dissolved in sterile water.^[3]

References

[1] Kobayashi M, et al. Pharmacological profiles of the potent carbonic anhydrase inhibitor dorzolamide hydrochloride, a topical antiglaucoma agent. Nihon Yakurigaku Zasshi. 2000, 115(6): 323-328. [2] Hasegawa T, et al. Binding of dorzolamide and its metabolite, N-deethylated dorzolamide, to human erythrocytes in vitro. Drug Metab Dispos. 1994, 22(3): 377-382. [3] Wang RF, et al. MK-507 (L-671,152), a topically active carbonic anhydrase inhibitor, reduces aqueous humor production in monkeys. Arch Ophthalmol. 1991, 109(9): 1297-1299.

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