1. GPCR/G Protein
  2. Adenosine Receptor
  3. A3AR modulator 1

A3AR modulator 1 (MRS8054) 是一种具有口服活性的 A3 腺苷受体 (A3AR (Adenosine Receptor)) 正变构调节剂 (PAM)。A3AR modulator 1 极大地增强了 Cl-IB-MECA 刺激的 [35S]GTPγS 结合 Emax

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A3AR modulator 1 Chemical Structure

A3AR modulator 1 Chemical Structure

CAS No. : 2991693-62-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [35S]GTPγS binding Emax[1].

IC50 & Target[1]

Adenosine A3 receptor

 

体外研究
(In Vitro)

A3AR modulator 1 (compound 39) shows a few weak off-target interactions, with Ki values of 0.123 μM, 0.891 μM, and 2.6 μM for translocator protein (TSPO), opioid receptor σ2, and 5HT2B receptor, respectively[1].

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

体内研究
(In Vivo)

In fasted Wistar rats, A3AR modulator 1 (compound 39) has considerably longer in vivo half-life and improved oral bioavailability (3.44 h, 64.0%F at 3 mg/kg; 3.84 h, 61.5%F at 10 mg/kg), indicating substantial oral bioavailability[1].

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

分子量

484.38

Formula

C23H25IN4

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
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  • 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:
A3AR modulator 1
目录号:
HY-151899
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