Brinzolamide

製品コードS3178 バッチS317801

印刷

化学情報

Synonyms

AL-4862

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₂H₂₁N₃O₅S₃

分子量

383.51

CAS No.

138890-62-7

Solubility (25°C)*

体外

DMSO

77 mg/mL (200.77 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (13.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/ml (1.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Brinzolamide (AL-4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.
in vivo	Brinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1–2 hours. This compound (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. This chemical at dosages of 30 mg/kg produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. It at 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice. ^[1] This compound (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of this chemical is 1%, and it is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily. ^[2] It significantly decreases intraocular pressure and arteriovenous passage time compared with placebo in healthy volunteers. ^[3] This compound (2%) increases optic nerve head blood flow and decreases intraocular pressure in tranquilized Dutch-belted rabbits. ^[4] It (1%) reduces intraocular pressure by reducing aqueous flow and not by affecting aqueous humor drainage in normotensive eyes of rabbits and hypertensive eyes of monkeys. ^[5]

製品説明

Brinzolamide (AL-4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.

in vivo

Brinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1–2 hours. This compound (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. This chemical at dosages of 30 mg/kg produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. It at 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice. ^[1] This compound (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of this chemical is 1%, and it is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily. ^[2] It significantly decreases intraocular pressure and arteriovenous passage time compared with placebo in healthy volunteers. ^[3] This compound (2%) increases optic nerve head blood flow and decreases intraocular pressure in tranquilized Dutch-belted rabbits. ^[4] It (1%) reduces intraocular pressure by reducing aqueous flow and not by affecting aqueous humor drainage in normotensive eyes of rabbits and hypertensive eyes of monkeys. ^[5]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/10665514/
https://pubmed.ncbi.nlm.nih.gov/10665517/
https://pubmed.ncbi.nlm.nih.gov/14736787/

https://pubmed.ncbi.nlm.nih.gov/10665515/
https://pubmed.ncbi.nlm.nih.gov/10779015/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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