Brinzolamide hydrochloride

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CAS NO:

150937-43-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

AL-4862 hydrochloride

产品介绍

Brinzolamide (AL-4862) hydrochloride 是一种选择性的碳酸酐酶 II（carbonic anhydrase II）抑制剂，其IC₅₀值为 3.2 nM。Brinzolamide hydrochloride 可以通过抑制睫状体 CA-II，降低房水分泌，从而降低眼压 (IOP)。可用于青光眼疾病的研究。

生物活性

Brinzolamide (AL-4862) hydrochloride is a selectivecarbonic anhydraseIIinhibitor with anIC₅₀value 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].

IC₅₀& Target^[1]

hCA II

3.2 nM (IC₅₀)

体内研究
(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
T_max(h)	0.08	0.5	1	0.25
C_max(ng/mL, ng/g)	11,050	1964	408	1245
Terminal t_1/2(h)	3.4	13	2	13.6
AUC_0-24h(hng/mL, hng/g)	17,780	7725	1896	11414
AUC_0-∞(hng/mL, hng/g)	17,836	8839	1955	16628
Dose-normalized AUC_0-∞(h/mL, h/g)	4	2	0.004	0.03

Animal Model:	Rabbits^[2]
Dosage:	7.5 mg, 12 mg
Administration:	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.

Clinical Trial

分子量

419.97

Formula

C₁₂H₂₂ClN₃O₅S₃

CAS 号

150937-43-2

中文名称

布林佐胺盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.