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

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

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MRS 5980

MRS 5980 Chemical Structure

CAS No. : 1639420-13-5

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MRS 5980 Related Antibodies

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Description

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

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]
Molecular Weight

458.92

Formula

C20H19ClN6O3S
CAS No.
SMILES

CNC([C@]12[C@]([C@@H](N3C4=NC(C#CC5=CC=C(S5)Cl)=NC(NC)=C4N=C3)[C@@H]([C@@H]2O)O)([H])C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MRS 5980 Related Classifications

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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.

Keywords:

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

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MRS 5980
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HY-156983
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