2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein
  3. Carbonic Anhydrase Adrenergic Receptor
  4. CAXII-IN-3

CAXII-IN-3 一种有效的碳酸酐酶 (CA XII) 抑制剂，其 Ki 为 53 nM。CAXII-IN-3 对多种人类 CA 亚型表现出选择性抑制作用，对 CA I、CA II、CA IV 和 CA IX 的 Ki 分别为 5.3 μM、75 nM、1.9 μM 和 > 10 μM。CAXII-IN-3 主要抑制 CA II 和 CA XII，从而减少房水的产生。CAXII-IN-3 具有 β3-AR 激动活性，可扩张视网膜血管，改善视神经灌注。CAXII-IN-3 可用于青光眼等眼部疾病的研究。

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CAXII-IN-3

CAXII-IN-3 Chemical Structure

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CAXII-IN-3 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

查看 Adrenergic Receptor 亚型特异性产品:

查看所有亚型
α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CAXII-IN-3 is an effective carbonic anhydrase (CA XII) inhibitor with a Ki of 53 nM. CAXII-IN-3 exhibits selective inhibition against multiple human CA subtypes with Kis of 5.3 μM, 75 nM, 1.9 μM, > 10 μM against CA I, CA II, CA IV and CA IX. CAXII-IN-3 mainly inhibits CA II and XII, and reduces aqueous humor production. CAXII-IN-3 exhibits β3-AR agonistic activity, can dilate retinal blood vessels, and improve optic nerve perfusion. CAXII-IN-3 can be used in the research of ocular disorders such as glaucoma[1].

IC50 & Target[1]

hCA XII

53 nM (Ki)

hCA II

75 nM (Ki)

hCA I

5.3 μM (Ki)

hCA IX

> 10 μM (Ki)

Beta-1 adrenergic receptor

 

Beta-2 adrenergic receptor

 

Beta-3 adrenergic receptor

 

体外研究
(In Vitro)

CAXII-IN-3 (Compound 14) (0.1 pM-10 μM) 可增加稳定表达 β1、β2 和 β3 肾上腺素能受体亚型的 HEK293T 细胞中的 cAMP 生成，pEC50 值分别为 5.00、5.29 和 4.98[1]。
CAXII-IN-3 (1 nM-0.1 μM, 0-50 min) 可诱导猪视网膜动脉环完全血管舒张，EC50 为 11 μM[1]。
CAXII-IN-3 (4 μM, 2 h) 在猪视网膜色素上皮 (RPE) 中表现出与 Propranolol (HY-B0573B) 相当的黑素体积累[1]。

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

CAXII-IN-3 相关抗体:
体内研究
(In Vivo)

CAXII-IN-3 (Compound 14) (30 μL 1% 溶液，滴眼，单剂量) 在给药后 120 分钟达到最大效果，可降低兔眼压 (IOP)[1]。

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

Animal Model: Instantaneous high intraocular pressure model established in New Zealand White (NZW) rabbits[1]
Dosage: 30 μL of 1% solution
Administration: Eye drip, single dose
Result: Produced the greatest and most sustained effect.
分子量

459.56

Formula

C26H25N3O3S
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

CAXII-IN-3 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:

CAXII-IN-3Carbonic AnhydraseAdrenergic ReceptorCarbonate dehydrataseBeta ReceptorDual-Targeting Ligandsβ3-Adrenergic Receptor AgonistsIntraocular PressureMelanin BindingOphthalmic PharmacokineticsInhibitorinhibitorinhibit

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目录号：
HY-178030
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