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    Dorzolamide HCl
    Dorzolamide HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0893
    CAS #: 130693-82-2Purity ≥98%

    Description: Dorzolamide HCl (also known as MK-507, or L-671152 HCl; L671152; MK507; trade name Trusopt) is a water-soluble, potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively, it is used as anti-glaucoma agent that is topically applied in the form of eye drops. Dorzolamide hydrochloride is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.

    References: J Ocul Pharmacol Ther. 1997 Feb;13(1):23-30; Vet Ophthalmol. 2001 Mar;4(1):61-7.

    Related CAS:120279-96-1 (free base)

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    Molecular Weight (MW)360.9
    FormulaC10H16N2O4S3.HCl
    CAS No.130693-82-2 (HCl); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: 14 mg/mL (38.79 mM)
    Ethanol: <1 mg/mL
    Other NameChemical Name: (4S,6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide hydrochloride
    InChi Key: OSRUSFPMRGDLAG-QMGYSKNISA-N
    InChi Code: InChI=1S/C10H16N2O4S3.ClH/c1-3-12-8-4-6(2)18(13,14)10-7(8)5-9(17-10)19(11,15)16;/h5-6,8,12H,3-4H2,1-2H3,(H2,11,15,16);1H/t6-,8-;/m0./s1
    SMILES Code: O=S(C(S1)=CC([[email protected]@H](NCC)C[[email protected]@H]2C)=C1S2(=O)=O)(N)=O.[H]Cl
    SynonymsDorzolamide; MK-507 (L-671152) HCl; L-671152; TRUSOPT; Dorzolamide HCI; Dorzolamide Hydrochloride; L 671152; L671152; MK-507; MK 507; MK507


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    In Vitro

    In vitro activity: Dorzolamide is a powerful inhibitor of carbonic anhydrase (CA) II that penetrates the sclera and cornea to reach the ciliary process and lowers formation of HCO3 and aqueous humor. Dorzolamide causes a vasodilatation of retinal arteries, pre-contracted by three different mechanisms by direct action and presumably independent of changes in extracellular pH.


    Kinase Assay: Dorzolamide(L671152; MK507) is an anti-glaucoma agent, which is a carbonic anhydrase inhibitor. Target: carbonic anhydrase (CA) Dorzolamide is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour. Glaucoma was induced in the right eye of adult Wistar rats by episcleral venous occlusion. One experimental group was administered dorzolamide 2%-timolol 0.5% combination eye drops, while the other experimental group was administered dorzolamide 2% eye drops. Control groups had surgery without drug administration. Drug application was initiated either 2 weeks before surgery (Group A), from the day of surgery (Group B), 2 weeks after surgery (Group C), or 4 weeks after surgery (Group D). RGCs were labeled by intratectal Fluorogold injections and counted from flat-mount preparations, and IOP was measured using Tonopen. Both dorzolamide-timolol combination and dorzolamide, when applied topically, significantly reduced IOP and improved RGC densities in experimental eyes when compared to control eyes. Earlier initiation, as well as longer duration of drug application, resulted in higher RGC densities. Clinical indications: Glaucoma; Ocular hypertension FDA Approved Date: 1995 Toxicity: Dizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest.

    In VivoDorzolamide, administered twice and three times daily, significantly decreases intraocular pressure (IOP) in glaucomatous dogs on the first day (twice daily 7.6 mmHg, and three times daily 16.4 mmHg) that is even greater by day 5 (twice daily 10.4 mmHg, and three times daily 13.9 mmHg). Dorzolamide (instilled in the drug eye for day 1 through to day 5) combined with oral methazolamide (administered from day 3 through to day 5) significantly lowers IOP in the eye on day 1, for day 3 and for all of day 5 for both eyes. Dorzolamide (2%) instilled three times daily produces similar IOP declines compared to the combination of oral methazolamide and 2% dorzolamide administered twice daily. Dorzolamide hydrochloride induces a very large IOP reduction and is found to be also well effective at night in rabbit. Dorzolamide maximally lowers the intraocular pressure (IOP) of glaucomatous monkeys by 22%, 30% and 37%, respectively.
    Animal model dogs
    Formulation & Dosage twice daily 7.6 mmHg, and three times daily 16.4 mmHg
    ReferencesJ Ocul Pharmacol Ther. 1997 Feb;13(1):23-30; Vet Ophthalmol. 2001 Mar;4(1):61-7.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Dorzolamide HCl

    The changes in optic nerve oxygen tension induced by injections of timolol, dorzolamide, dorzolamide after timolol, and a combination of dorzolamide and timolol. Br J Ophthalmol. 2004 Feb; 88(2): 276–279.
     

    Dorzolamide HCl

    Optic nerve oxygen tension in kPa over time during different kinds of manipulations. Br J Ophthalmol. 2004 Feb; 88(2): 276–279.
     

    Dorzolamide HCl

    A) Bilateral eczematous periorbital swelling after instillation of dorzolamide eyedrops. (B) Improved periorbital swelling after cessation of dorzolamide eyedrops. Clin Ophthalmol. 2015; 9: 575–577.


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