2. GPCR/G Protein
  3. Adenosine Receptor
  4. MRS7469

MRS7469 是一种高选择性 A1 腺苷受体 (A1AR) 激动剂，对其他腺苷受体亚型的选择性超过 2000 倍。MRS7469 稳定结合 A1AR 的正构结合位点，对人及小鼠均表现出极高的亲和力 (如人 pKi 为 8.67，小鼠 pKi 为 9.43)。MRS7469 通过激活中枢 A1AR，可显著诱导体温降低、运动抑制及精神运动功能障碍，可广泛应用于抑郁症等相关领域的研究。

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MRS7469

MRS7469 Chemical Structure

CAS No. : 2257428-48-9

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MRS7469 相关抗体

Top Publications Citing Use of Products

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pKi is 8.67, mouse pKi is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields[1][2][3].

IC50 & Target[1]

hA1AR

2.14 nM (Kd)

体外研究
(In Vitro)

MRS7469 对 hA1AR (pKi=8.67) 和 mA1AR (pKi=9.43) 表现出高结合亲和力，而对 hA2AAR、hA3AR 及 mA3AR 的亲和力则低得多[2]。
MRS7469 靶向 hA1AR 的结合亲和力为 2.14 nM，对其他腺苷受体亚型的选择性超过 2000 倍[3]。

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

MRS7469 相关抗体:
体内研究
(In Vivo)

MRS7469 (52 µg/kg；侧脑室注射) 经外周给药时，优先激活中枢 A1 腺苷受体而非外周 A3 腺苷受体，诱导 A1 腺苷受体依赖性低体温和运动抑制；并会引发严重低体温[2]。

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

Animal Model: Mice[2]
Dosage: 52 µg/kg (i.c.v.)
Administration: i.c.v.
Result: Induced intense hypothermia.
Activated central A1 adenosine receptors preferentially over peripheral A3 adenosine receptors, leading to A1 adenosine receptor-dependent hypothermia and locomotor depression.
Exhibited a high affinity for mouse A1 adenosine receptors (Ki=0.37 nM).
Crossed the blood-brain barrier sufficiently to activate central A1 adenosine receptors.
分子量

433.93

Formula

C21H28ClN5O3
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

MRS7469 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

MRS74692257428-48-9MRS 7469MRS-7469Adenosine ReceptorP1 receptorA2AARadenosine receptor subtypesmolecular dynamics simulationA1ARA1 adenosine receptorlocomotor depressionhypothermiapsychomotor dysfunctionblood-brain barrierdepressionInhibitorinhibitorinhibit

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