Brinzolamide

SKU: B0424

Category: API's & Intermediates

Synonyms: (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide , AL 4862 , Azopt; 138890-62-7
CAS-Number: C₁₂H₂₁N₃O₅S₃
Molecular Formula: 383.51
Molecular Weight

Product Data
Handling
Safety Information
Details

Specifications

Purity: ≥98% (HPLC)
Identity: 1H-NMR
Appearance: White to beige powder

Properties

Solvents: DMSO (30mg/ml), water or ethanol (insoluble)

Short Term Storage: -20°C
Use / Stability: Stable for at least 2 years after receipt when stored at -20°C.
Handling Advice: Protect from light and moisture.
Long Term Storage: -20°C
Shipping: AMBIENT

Transportation: Not dangerous goods

Description: Brinzolamide is a potent inhibitor of carbonic anhydrases (IC50=3.2nM and 45.3nM for CAII and CAIV, respectively) that lowers intraocular pressure by locally inhibiting carbonic anhydrase in the ciliary processes and suppressing aqueous humor secretion. Animal studies have found that one week of twice-daily topical ocular treatment with 2% brinzolamide significantly reduced IOP and enhanced optic nerve head blood flow.
References: (1) T. Stams, et al., Protein Science 7, 556 (1998) , (2) P.A. Boriack-Sjodin, et al., Protein Science 7, 2483 (1998) , (3) C.J. Ingram & R.F. Brubaker, Am. J. Ophthalmol. 128, 292 (1999) , (4) G.E. Barnes, et al., Survey of Ophthalmol. 44, S131 (2012) , (5) H. Zheng & B. Lou, Acta Crystallogr. E Crystallogr. Commun. 72, 692 (2016) , (6) T. Nakano, et al., Adv. Ther. 33, 1452 (2016) , (7) Y.R. Dong, et al., Int. J. Ophthalmol. 11, 719 (2018)
InChi Key: HCRKCZRJWPKOAR-JTQLQIEISA-N
Smiles: O=S(C1=CC2=C(S1)S(N(CCCOC)C[C@@H]2NCC)(=O)=O)(N)=O

Brinzolamide is a potent inhibitor of carbonic anhydrases (IC50=3.2nM and 45.3nM for CAII and CAIV, respectively) that lowers intraocular pressure by locally inhibiting carbonic anhydrase in the ciliary processes and suppressing aqueous humor secretion. Animal studies have found that one week of twice-daily topical ocular treatment with 2% brinzolamide significantly reduced IOP and enhanced optic nerve head blood flow.

Artikelnummer: B0424 Kategorie: API's & Intermediates

Zusätzliche Information

Zusätzliche Information

Synonyms	(R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide, AL 4862, Azopt
Purity	≥98% (HPLC)
Appearance	White to beige powder
CAS-Number	138890-62-7
Molecular Formula	C12H21N3O5S3
Molecular Weight	383.51
Identity	1H-NMR
Solvents	DMSO (30mg/ml), water or ethanol (insoluble)
Smiles	O=S(C1=CC2=C(S1)S(N(CCCOC)C[C@@H]2NCC)(=O)=O)(N)=O
InChi Key	HCRKCZRJWPKOAR-JTQLQIEISA-N
Shipping	AMBIENT
Short Term Storage	-20°C
Long Term Storage	-20°C
Handling Advice	Protect from light and moisture.
Use / Stability	Stable for at least 2 years after receipt when stored at -20°C.
Transportation	Not dangerous goods
References	(1) T. Stams, et al., Protein Science 7, 556 (1998), (2) P.A. Boriack-Sjodin, et al., Protein Science 7, 2483 (1998), (3) C.J. Ingram & R.F. Brubaker, Am. J. Ophthalmol. 128, 292 (1999), (4) G.E. Barnes, et al., Survey of Ophthalmol. 44, S131 (2012), (5) H. Zheng & B. Lou, Acta Crystallogr. E Crystallogr. Commun. 72, 692 (2016), (6) T. Nakano, et al., Adv. Ther. 33, 1452 (2016), (7) Y.R. Dong, et al., Int. J. Ophthalmol. 11, 719 (2018)
Quantity	10 mg, 50 mg, Bulk