2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Carbonic Anhydrase Apoptosis NOD-like Receptor (NLR)
  4. CAII-IN-15

CAII-IN-15 是一种强效的碳酸酐酶 II (CA II) 抑制剂，其对 hCA II 的 IC50 为 10 nM。CAII-IN-15 可提高 cGMP 水平、释放一氧化氮、减轻氧化应激，并在体外展现出神经保护活性。CAII-IN-15 可抑制 NLRP3 炎症小体活化、减少神经元凋亡 (apoptosis)。CAII-IN-15 可降低兔的眼内压 (IOP)。CAII-IN-15 可用于青光眼的相关研究。

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CAII-IN-15

CAII-IN-15 Chemical Structure

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CAII-IN-15 相关抗体

Top Publications Citing Use of Products

查看 Carbonic Anhydrase 亚型特异性产品:

查看所有亚型
CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

查看 NOD-like Receptor (NLR) 亚型特异性产品:

查看所有亚型
NLRP3 NLRP1 NOD1 NOD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CAII-IN-15 is a potent carbonic anhydrase II (CA II) inhibitor with a hCA II IC50 of 10 nM. CAII-IN-15 elevates cGMP levels, releases nitric oxide, reduces oxidative stress, and exhibits neuroprotective activity in vitro. CAII-IN-15 inhibits NLRP3 inflammasome activation, reduces neuronal apoptosis. CAII-IN-15 reduces Intraocular pressure (IOP) in rabbits. CAII-IN-15 can be used for the research of glaucoma[1].

IC50 & Target[1]

hCA II

10 nM (IC50)

hCA IX

32 nM (IC50)

hCA I

430 nM (IC50)

hCA XII

19 nM (IC50)

NLRP3 inflammasome

 

体外研究
(In Vitro)

CAII-IN-15 (compound B6) (0.5 nM-5 mM; 15 min) 可强效且选择性地抑制重组人 CA II，其 IC50 为 10 nM；同时对 hCA I (IC50 = 430 nM)、hCA IX (IC50 = 32 nM) 和 hCA XII (IC50 = 19 nM) 表现出中等抑制活性[1]。
CAII-IN-15 通过 Zn2+ 配位、与 THR199 和 GLN92 形成氢键以及与 PHE131 发生 π-π 堆积作用结合于 CA II 的活性位点，这一作用支撑了其强效抑制活性[1]。
CAII-IN-15 (10 μM; 24 h) 可升高人小梁网 (HTM) 细胞内的 cGMP 水平，证实其可激活 NO/sGC/cGMP 信号通路[1]。
CAII-IN-15 (5-20 μM; 4 h) 对氧糖剥夺 (OGD) 诱导的 SH-SY5Y 细胞损伤具有浓度依赖性神经保护作用[1]。
CAII-IN-15 (10 μM; 24 h) 可抑制 LPS (HY-D1056) 诱导的 Müller 细胞中 IL-1β 和 NLRP3 炎症小体的表达升高[1]。
CAII-IN-15 (10 μM; 4 h) 可抑制视网膜前体细胞 R28 中由 OGD/R 诱导的 ROS 水平升高[1]。
CAII-IN-15 (0.032-100 μM; 24 h) 在多种眼细胞类型中表现出剂量依赖性细胞毒性[1]。
CAII-IN-15 (1.56-50.00 μg/mL; 1 h) 在 1.56 μg/mL 至 50.00 μg/mL 的浓度下对兔红细胞无显著溶血活性，溶血率持续低于 5%，显示出优良的血液相容性[1]。
CAII-IN-15 (0-30 μM) 在最高 30 μM 的浓度下对 hERG 钾通道无显著抑制作用，提示心律失常风险较低且心脏安全性良好[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CAII-IN-15 相关抗体:

ELISA Assay[1]

Cell Line: human trabecular meshwork (HTM) cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly Increased intracellular cGMP levels to approximately 15.8 nmol/L.

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 5; 10; 20 μM
Incubation Time: 4 h
Result: Restored OGD-reduced cell viability to 88.10% (5 μM), 91.12% (10 μM), and 93.71% (20 μM).
Showed concentration-dependent neuroprotection.

ELISA Assay[1]

Cell Line: lipopolysaccharide (LPS)-stimulated Müller cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Substantially reduced LPS-induced ASC speck counts and IL-1β concentrations.

Cell Viability Assay[1]

Cell Line: conjunctival cells, human corneal epithelial cells (HCEC), human trabecular meshwork cells (HTMC), lens B3 cells, retinal R28 cells, and 661W cells
Concentration: 0.032; 0.16; 0.8; 4 μM (conjunctival cells); 0.8; 4; 20; 100 μM (HCEC, HTMC, B3, R28, 661W cells)
Incubation Time: 24 h
Result: Decreased conjunctival cell viability from 97.76% to 76.76% across tested concentrations, with 15.09% higher viability than brinzolamide at 0.032 μM.
Decreased HCEC viability from 99.67% to 76.00%, with 5.33% higher viability than brinzolamide at 100 μM.
Decreased HTMC viability from 99.83% to 91.00%, with 3.73% higher viability than brinzolamide at 4 μM.
Decreased B3 cell viability from 99.67% to 90.33%, with 3.09% higher viability than brinzolamide at 4 μM.
Decreased R28 cell viability from 95.90% to 70.67%, with 7.10% higher viability than brinzolamide at 4 μM.
Decreased 661W cell viability from 91.71% to 75.97%, with 10.86% higher viability than brinzolamide at 4 μM.
体内研究
(In Vivo)

CAII-IN-15 (compound B6) (0.05 mL 1% Carbomer 混悬液；眼部 (结膜囊滴注)；单次给药；或每日 2 次，连续给药 28 天) 在兔体内展现出急性和慢性降眼压 (IOP) 功效[1]。
CAII-IN-15 (0.1 mL 1% Carbomer 混悬液；经结膜囊局部滴注；单剂量) 在兔眼中表现出极低的眼刺激性[1]。
CAII-IN-15 (100 μL 1% 溶液；局部 (眼内滴注)；单次给药) 可在兔房水中释放一氧化氮[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male New Zealand white rabbits ( 2-3 months old, 2-2.5 kg) bilateral intravitreally injected with 0.05 mL 5% hypertonic saline[1]
Dosage: 0.05 mL in 1% carbomer suspension
Administration: topical (conjunctival sac instillation); single dose
Result: Achieved a maximum IOP reduction of -6.5 mmHg at 30 minutes post-administration.
Exhibited sustained efficacy lasting until 240 minutes.
Animal Model: Male New Zealand white rabbits ( 2-3 months old, 2-2.5 kg) bilateral intravitreally injected with with 0.1 mL Carbomer (HY-W250721D)[1]
Dosage: 0.05 mL in1% carbomer suspension
Administration: topical (conjunctival sac instillation); twice daily; 28 days
Result: Provided consistent additional IOP reduction throughout the core observation period (days 10-26), with peak differences of 3.0 mmHg recorded on days 14 and 17.
Animal Model: Male New Zealand white rabbits ( 2-3 months old, 2-2.5 kg)[1]
Dosage: 0.1 mL in 1% carbomer suspension
Administration: topical (conjunctival sac instillation); single dose
Result: At 1 hour post-instillation, showed mild conjunctival hyperemia and minimal secretion with a total irritation score of 0.75.
Scores returned to baseline (0) by 2 hours.
Classified as a non-irritant (maximum score ≤1).
Animal Model: Male New Zealand white rabbits ( 2-3 months old, 2-2.5 kg)[1]
Dosage: 1% solution, 100 μL
Administration: topical (ocular instillation); single dose
Result: Released nitric oxide at a concentration of 5.75-6.21 μM at 0.5 hour post-administration.
Decreased Nitric oxide release sharply at 1 hour and 1.5 hours post-administration.
分子量

351.33

Formula

C14H13N3O6S
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.
纯度 & 产品资料
参考文献

CAII-IN-15 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CAII-IN-15Carbonic AnhydraseApoptosisNOD-like Receptor (NLR)Carbonate dehydrataseCYP1A2human trabecular meshwork cellsNLRP3 inflammasomeSH-SY5Y cellsMüller cellshuman CA IIrabbit erythrocytesretinal precursor R28 cellscarbonic anhydrase IIhERG potassium channelInhibitorinhibitorinhibit

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