1. GPCR/G Protein
  2. Adenosine Receptor
  3. MRS5698

MRS5698 是一种选择性 Gi 蛋白偶联 A3 腺苷受体 (A3AR) 激动剂,对于人和小鼠 A3AR 的 Ki 约为 3 nM。MRS5698 可用于疼痛和银屑病的研究。

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MRS5698 Chemical Structure

MRS5698 Chemical Structure

CAS No. : 1377273-00-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis[1][2].

IC50 & Target[1]

Adenosine A3 receptor

~3 nM (Ki)

体外研究
(In Vitro)

MRS5698 displays higher affinity and selectivity (>3000-fold) agonist A3R vs. other adenosine receptor (ARs) in both human and mouse[1].
MRS5698 (0.1-10 µM; 1 hours) induces a concentration-dependently robust A3R-mediated cAMP reduction in HEK-293T cells permanently expressing the A3R, regardless the illumination condition[3].

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

体内研究
(In Vivo)

MRS5698 (3 nmol/day; intrathecal injection for 25 days) prevents Oxaliplatin-induced mechano-allodynia and hyperalgesia, and attenuates Oxaliplatin-induced NLRP3/IL-1β neuroinflammation[2].
MRS5698 (1 mg/kg; i.p. at days 2, 3 ) reduces the IL-23 induced (IL23 injected in day 0, 1, 3) ear thickness of C57BL/6N mouse during the third and fourth experimental days[3].

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

Animal Model: Oxaliplatin-induced Male Sprague Dawley rats (200–250 g starting weight)[2]
Dosage: 3 nmol/day
Administration: Intrathecal injection for 25 days
Result: Increased the value of mechanical paw withdrawal threshold in grams (PWT) in rat.
Attenuated oxaliplatin-induced expression of NLRP3 and maturation of caspase 1 in the DH-SC.
Reduced IL-1β levels in the spinal cord.
分子量

564.97

Formula

C28H23ClF2N6O3

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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  • 稀释计算器

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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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MRS5698
目录号:
HY-110202
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