150937-43-2

150937-43-2 structure

Name: (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide,hydrochloride
Chemical Name: (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide,hydrochloride
CAS Number: 150937-43-2
Molecular Formula: C₁₂H₂₂ClN₃O₅S₃
Molecular Weight: 419.96800
Catalog: Signaling Pathways Metabolic Enzyme/Protease Carbonic Anhydrase
Create Date: 2017-06-04 12:05:54
Modify Date: 2024-01-12 00:42:28
Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research[1][2].

Name	(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide,hydrochloride
Synonyms	Azopt Hydrochloride UNII-N36YTS80H4 AL-4682 Hydrochloride Brinzolamide Hydrochloride

Description	Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research[1][2].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase Research Areas >> Neurological Disease
Target	IC50: 3.2 nM (carbonic anhydrase II)[2].
In Vivo	Brinzolamide (7.5 mg or 12 mg) hydrochloride implanted in a silicone matrix is extremely well tolerated and provides sustained release of brinzolamide and significant reduction in intraocular pressure (IOP) for up to 28 days with no adverse effects or signs of toxicity in normotensive NZW rabbits[2]. The pharmacokinetic parameters of Brinzolamide hydrochloride in rabbits[1]. Intracameral Administration (4.5 mg) Intracameral Administration (4.5 mg) Topical Administration (500 mg) Topical Administration (500 mg) PK Parameters Aqueous Humor Iris-Ciliary Body Aqueous Humor Iris-Ciliary Body Tmax (h) 0.08 0.5 1 0.25 Cmax (ng/mL, ng/g) 11,050 1964 408 1245 Terminal t1/2 (h) 3.4 13 2 13.6 AUC0-24h (hng/mL, hng/g) 17,780 7725 1896 11414 AUC0-∞ (hng/mL, hng/g) 17,836 8839 1955 16628 Dose-normalized AUC0-∞ (h/mL, h/g) 4 2 0.004 0.03 Animal Model: Rabbits[2] Dosage: 7.5 mg, 12 mg Administration: Brinzolamide silicone matrix implant placed in the episcleral space Result: Resulted in a significant IOP reduction of 4.6 mmHg on days 10-28, with concentrations of 12 mg.
References	[1]. Vatsala Naageshwaran, et al. Comprehensive Ocular and Systemic Pharmacokinetics of Brinzolamide in Rabbits After Intracameral, Topical, and Intravenous Administration. J Pharm Sci. 2021 Jan;110(1):529-535. [2]. Sara M.Smith, et al. Tolerability, pharmacokinetics, and pharmacodynamics of a brinzolamide episcleral sustained release implant in normotensive New Zealand white rabbits,Journal of Drug Delivery Science and Technology,Volume 61,2021,102123,ISSN 1773-2247

Boiling Point	586ºC at 760 mmHg
Molecular Formula	C₁₂H₂₂ClN₃O₅S₃
Molecular Weight	419.96800
Flash Point	308.2ºC
Exact Mass	419.04100
PSA	163.80000
LogP	4.07960
Vapour Pressure	1.03E-13mmHg at 25°C

1072782-87-6

~97%

150937-43-2

Literature: Duke Chem, S. A. Patent: EP1985618 A1, 2008 ; Location in patent: Page/Page column 11 ;

Precursor 1
1072782-87-6
DownStream 1
138890-62-7

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