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#	10-101-134
CAS	138890-62-7
Background	Brinzolamide is a highly specific carbonic anhydrase (CA) inhibitor which lowers intraocular pressure (IOP) by reducing the rate of aqueous humour formation. Formulated as a 1% ophthalmic suspension (Azopt) and administered twice or three times daily, brinzolamide is indicated for the topical management of primary open-angle glaucoma (POAG) and ocular hypertension (OH) as either monotherapy or adjunctive therapy with topical beta-blockers.
Synonyms/Alias	AGN-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
Chemical Name	(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide
M.F/Formula	C12H21N3O5S3
M.W/Mr.	383.51
Labeling Target	Carbonic Anhydrase
Application	Glaucoma Ocular hypertension
Appearance	Solid powder
Purity	>98% (or refer to the Certificate of Analysis)
Activity	Inhibitor
Areas of Interest	Cardiovascular System & Diseases Pituitary & Hypothalamic Hormones
Functions	Zinc ion binding
Target	Carbonic Anhydrase

CAT#	Product Name	M.W	Molecular Formula	Inquiry
10-101-113	Carbocysteine	179.19	C5H9NO4S	Inquiry
10-101-135	Carbidopa	226.23 (net); 244.25 (monohydrate)	C10H14N2O4	Inquiry
10-101-42	Carbetocin Acetate	1048.21	C47H73N11O14S	Inquiry
10-101-74	CCK-4 Acetate	596.71	C29H36N6O6S	Inquiry

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Source#	Synthetic
Solubility	Soluble in DMSO, not in water
Shipping Condition	Shipped 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 Conditions	Dry, dark and at 0 - 4 °C
Long-term Storage Conditions	-20 °C
Organism	Human
InChI	InChI=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 Key	HCRKCZRJWPKOAR-JTQLQIEISA-N
Canonical SMILES	CCNC1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
Isomeric SMILES	CCN[C@H]1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
BoilingPoint	586.0±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 (Azopt^TM), 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 Point	N/A