2. GPCR/G Protein
  3. Adenosine Receptor
  4. MRS 5980

MRS 5980 是一种口服有效的 A3AR 激动剂，Ki 为 0.7 nM。

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MRS 5980

MRS 5980 Chemical Structure

CAS No. : 1639420-13-5

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MRS 5980 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

MRS 5980 is an A3AR agonist with a Ki value of 0.7 nM. MRS 5980 has oral activity[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.6 nM
Compound: 33
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
[PMID: 25422861]
HEK293 EC50
1180 nM
Compound: 1; MRS5980
Enhancing of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
Enhancing of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 EC50
131 nM
Compound: 1; MRS5980
Enhancing of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
Enhancing of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 EC50
35.1 nM
Compound: 1; MRS5980
Enhancing of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
Enhancing of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 EC50
> 10 μM
Compound: 1; MRS5980
Enhancing of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
Enhancing of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 EC50
> 10 μM
Compound: 1; MRS5980
Enhancing of [3H]mazindol binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
Enhancing of [3H]mazindol binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 EC50
> 10 μM
Compound: 1; MRS5980
Enhancing of [3H]mazindol binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
Enhancing of [3H]mazindol binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 IC50
253 nM
Compound: 1; MRS5980
Inhibition of recombinant human DAT expressed in HEK293 cell membranes assessed as reduction in [3H]-DA uptake incubated for 22 mins by micro beta scintillation counting analysis
Inhibition of recombinant human DAT expressed in HEK293 cell membranes assessed as reduction in [3H]-DA uptake incubated for 22 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 IC50
36 μM
Compound: 10
Binding affinity to mouse adenosine A3 receptor expressed in HEK293 cell membranes
Binding affinity to mouse adenosine A3 receptor expressed in HEK293 cell membranes
[PMID: 26191370]
HEK293 IC50
8.5 μM
Compound: 10
Binding affinity to canine adenosine A3 receptor expressed in HEK293 cell membranes
Binding affinity to canine adenosine A3 receptor expressed in HEK293 cell membranes
[PMID: 26191370]
HEK293 IC50
> 10 nM
Compound: 1; MRS5980
Inhibition of recombinant human SERT expressed in HEK293 cell membranes assessed as reduction in [3H]5-HT uptake incubated for 22 mins by micro beta scintillation counting analysis
Inhibition of recombinant human SERT expressed in HEK293 cell membranes assessed as reduction in [3H]5-HT uptake incubated for 22 mins by micro beta scintillation counting analysis
[PMID: 28319392]
HEK293 IC50
> 10 μM
Compound: 1; MRS5980
Inhibition of recombinant human NET expressed in HEK293 cell membranes assessed as reduction in [3H]-norepinephrine uptake incubated for 22 mins by micro beta scintillation counting analysis
Inhibition of recombinant human NET expressed in HEK293 cell membranes assessed as reduction in [3H]-norepinephrine uptake incubated for 22 mins by micro beta scintillation counting analysis
[PMID: 28319392]
分子量

458.92

Formula

C20H19ClN6O3S
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

MRS 5980 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:

MRS 59801639420-13-5MRS5980MRS-5980Adenosine ReceptorP1 receptorA3AR AgonistInhibitorinhibitorinhibit

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产品名称：
MRS 5980
目录号：
HY-156983
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