Brinzolamide

製品コードS3178 バッチS317801

印刷

化学情報

 Chemical Structure 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)
Clear solution
5% DMSO 95% corn oil
0.5mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml 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. 
* <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. Brinzolamide (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. Brinzolamide 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. Brinzolamide of 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] Brinzolamide (< 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 brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily. [2] Brinzolamide significantly decreases intraocular pressure and arteriovenous passage time compared with placebo in healthy volunteers. [3] Brinzolamide (2%) increases optic nerve head blood flow and decreases intraocular pressure in tranquilized Dutch-belted rabbits. [4] Brinzolamide (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)

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Hi-C profiling in tissues reveals 3D chromatin-regulated breast tumor heterogeneity and tumor-specific looping-mediated biological pathways [ bioRxiv, 2024, 2024.03.13.584872] PubMed: 38559097
Icariin regulates acidic microenvironment to alleviate pain caused by postmenopausal osteoporosis in the elderly [ Chinese Journal of Tissue Engineering Research, 2024, (28): 4461-4468.] PubMed: none
A Comparative Study of Drug Affinities Determined by Thermofluor and Kinetic Analysis [ ETD, 2020, N/A] PubMed: N/A
Evaluation of pentablock co-polymer (PTSsol) for sustained topical ocular drug delivery [Sara M.Smith, et al. J Drug Deliv Sci Tec, 2017, 10.1016/j.jddst.2017.05.005]

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。