Brinzolamide

    Brinzolamide is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

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    CAT No: 10-101-134

    CAS No: 138890-62-7

    Chemical Name: (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide

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    Specification Technical Data Publications Customer reviews and Q&A
    Synonyms/AliasAGN-190342; AL-4862; AL 4862; AL4862; UK-14304; (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide(R)-4-Ethylamino-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-thieno[3,2-e][1,2]thiazine-6-sulfonic acid amide
    M.F/FormulaC12H21N3O5S3
    M.W/Mr.383.51
    Labeling TargetCarbonic Anhydrase
    ApplicationGlaucoma Ocular hypertension
    AppearanceSolid powder
    Purity>98% (or refer to the Certificate of Analysis)
    ActivityInhibitor
    Areas of InterestCardiovascular System & Diseases
    Pituitary & Hypothalamic Hormones
    FunctionsZinc ion binding
    TargetCarbonic Anhydrase
    Source#Synthetic
    Long-term Storage ConditionsSoluble in DMSO, not in water
    Shipping ConditionShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
    Short-term Storage ConditionsDry, dark and at 0 - 4 °C
    Solubility-20 °C
    OrganismHuman
    InChIInChI=1S/C12H21N3O5S3/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17)/t10-/m0/s1
    InChI KeyHCRKCZRJWPKOAR-JTQLQIEISA-N
    Canonical SMILESCCNC1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
    Isomeric SMILESCCN[C@H]1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
    BoilingPoint586.0±60.0 °C at 760 mmHg
    ShelfLife>2 years if stored properly
    References

    Brinzolamide is a novel carbonic anhydrase inhibitor that elicits an ocular hypotensive effect when instilled topically. A multicenter, double-masked, placebo-controlled, parallel trial was conducted to evaluate the optimal intraocular pressure (IOP)-lowering concentration and ocular tolerability of topically administered brinzolamide (0.3%, 1%, 2%, and 3%) in patients with primary, open-angle glaucoma or ocular hypertension.

    Silver L H, Brinzolamide Dose-Response Study Group. Dose-response evaluation of the ocular hypotensive effect of brinzolamide ophthalmic suspension (Azopt®)[J]. Survey of ophthalmology, 2000, 44: S147-S153.

    To assess the effects of brinzolamide and dorzolamide on ocular haemodynamics and retinal oxygen saturation in patients with primary open-angle glaucoma (OAG). This pilot study suggests that brinzolamide and dorzolamide may increase retinal oxygen saturation in patients with OAG.

    Siesky B, Harris A, Cantor L B, et al. A comparative study of the effects of brinzolamide and dorzolamide on retinal oxygen saturation and ocular microcirculation in patients with primary open-angle glaucoma[J]. British journal of ophthalmology, 2008, 92(4): 500-504.

    Brinzolamide 1.0% produced clinically relevant intraocular pressure reductions in substantial numbers of patients. Brinzolamide's effectiveness equaled that of dorzolamide 2.0% and it produced less ocular discomfort (burning and stinging) on instillation.

    Silver L H, Group T B P T S. Clinical efficacy and safety of brinzolamide (AzoptTM), a new topical carbonic anhydrase inhibitor for primary open-angle glaucoma and ocular hypertension[J]. American journal of ophthalmology, 1998, 126(3): 400-408.

    Melting PointN/A

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