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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- CAS No.: 1639420-13-5
- Formule: C20H19ClN6O3S
- Masse moléculaire:458.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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 |
>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 | 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 | 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] |
| 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] |
Chemical Information
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CAS No. 1639420-13-5
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Masse moléculaire 458.92
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Formule C20H19ClN6O3S
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Select Batch:
Pureté:
99.98%
Assay:
99.98%
ee.:
99.98%
Références
Calculators
Calculateur de molarité
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Calculateur de dilution
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRS 5980 Related Classifications
HY-156983 Related Classifications
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