1. GPCR/G Protein
  2. Adenosine Receptor
  3. Adenosine receptor inhibitor 1

Adenosine receptor inhibitor 1 

目录号: HY-147907
产品使用指南

Adenosine receptor inhibitor 1 是一种有效的选择性腺苷受体 (adenosine receptor (AR)) 抑制剂,A1AR、A2AAR、A2BAR、A3AR 的 Ki 值 分别为 >1000, 68.5, >1000, >1000 nM。Adenosine receptor inhibitor 1 显示出镇痛活性、抗炎作用和外周镇痛作用。Adenosine receptor inhibitor 1具有研究癌症或神经退行性疾病的潜力。

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Adenosine receptor inhibitor 1 Chemical Structure

Adenosine receptor inhibitor 1 Chemical Structure

CAS No. : 2550400-52-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].

IC50 & Target[1]

A1AR

>1000 nM (Ki)

A2AR

68.5 nM (Ki)

hA2B

>1000 nM (Ki)

Adenosine A3 receptor

>1000 nM (Ki)

体外研究
(In Vitro)

Adenosine receptor inhibitor 1 (compound 12d) (120 min) shows metabolic stability incubated with with 96.56 and 97.97% of the parent compound remained in the reaction mixtures after incubation with mouse (MLMs) and rat liver microsomes (RLMs), respectively[1].

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

体内研究
(In Vivo)

Adenosine receptor inhibitor 1 (20, 30, 40 mg/kg; i.p.) shows antinociceptive activity at a concentration-dependent mannner[1].
Adenosine receptor inhibitor 1 (20 mg/kg; i.p.) shows anti-inflammatory effect in carrageenan-induced edema model[1].
Adenosine receptor inhibitor 1 (5, 10, 20 mg/kg; i.p.) shows analgesic effect in mouse[1].

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

Animal Model: 18-26 g male albino Swiss mice (chronic pain induced by the administration of 5% formalin) [1]
Dosage: 20, 30, 40 mg/kg
Administration: I.p.
Result: Showed antinociceptive activity with decreasesed the licking/biting time of the right hind paw of mice in response to the irritating chemical stimulus.
Animal Model: 150-180 g male rats Wistar(carrageenan-induced edema model)[1]
Dosage: 20 mg/kg
Administration: I.p.
Result: Showed anti-inflammatory effect with the inhibition of 23.3%, 54.2%, 66.0% at 1h, 2h, 3h, respectively.
Animal Model: Mouse (induce pain of peripheral origin by injection of an irritant like phenylbenzoquinone or acetic acid in mice)[1]
Dosage: 5, 10, 20 mg/kg
Administration: I.p.
Result: Showed peripheral analgesic effect with the significant decrease in the number of writhings by 32.9%, 54.9%, 82.0% at doses of 5, 10, 20 mg/kg, respectively.
分子量

395.82

Formula

C17H19ClFN5O3

CAS 号
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

Adenosine receptor inhibitor 1 相关分类

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  • 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 *
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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.

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产品名称:
Adenosine receptor inhibitor 1
目录号:
HY-147907
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