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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1639420-13-5
- 分子式: C20H19ClN6O3S
- 分子量:458.92
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Adenosine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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] |
化学情報
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CAS 番号 1639420-13-5
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分子量 458.92
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
バッチを選択:
純度:
99.98%
Assay:
99.98%
ee.:
99.98%
参考文献
Calculators
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希釈計算機
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MRS 5980 関連分類
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