MGS0039
MGS0039 is a type II group mGluR antagonist. MGS0039 has a high affinity for mGluR2 and mGluR3, with Ki values of 2.2 nM and 4.5 nM, respectively. MGS0039 can attenuate the inhibitory effect of glutamate-induced cyclic AMP formation triggered by Forskolin (HY-15371) in CHO cells expressing mGluR2/mGluR3. MGS0039 shows antidepressant-like activity in rats.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 569686-87-9
- 分子式: C15H14Cl2FNO5
- 分子量:378.18
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>100000 nM
Compound: (-)-11be
|
Effective concentration for agonistic activity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells
Effective concentration for agonistic activity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | EC50 |
>100000 nM
Compound: (-)-11be
|
Effective concentration for agonistic activity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells
Effective concentration for agonistic activity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | EC50 |
>100000 nM
Compound: (-)-11be
|
Effective concentration for agonistic activity towards metabotropic glutamate receptor 5 of rat expressed in CHO cells
Effective concentration for agonistic activity towards metabotropic glutamate receptor 5 of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | EC50 |
>100000 nM
Compound: (-)-11be
|
Effective concentration for agonistic activity towards metabotropic glutamate receptor 6 of rat expressed in CHO cells
Effective concentration for agonistic activity towards metabotropic glutamate receptor 6 of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | IC50 |
11700 nM
Compound: (-)-11be
|
Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells
Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | IC50 |
1740 nM
Compound: (-)-11be
|
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | IC50 |
20 nM
Compound: (-)-11be
|
Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells
Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | IC50 |
2060 nM
Compound: (-)-11be
|
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | IC50 |
24 nM
Compound: (-)-11be
|
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | IC50 |
93300 nM
Compound: (-)-11be
|
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | EC50 |
>100000 nM
Compound: (-)-11be
|
Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells
Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells
|
[PMID: 15317467] |
| CHO | IC50 |
20 nM
Compound: MGS0039
|
Antagonist activity at mGLUR2 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production
Antagonist activity at mGLUR2 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production
|
[PMID: 22318160] |
| CHO | IC50 |
24 nM
Compound: MGS0039
|
Antagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production
Antagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production
|
[PMID: 22318160] |
化学情報
-
CAS 番号 569686-87-9
-
分子量 378.18
-
分子式 C15H14Cl2FNO5
-
SMILES
O=C(O)[C@]1([C@@]2([C@](F)([C@@]2(C[C@H]1OCC3=CC=C(C(Cl)=C3)Cl)[H])C(O)=O)[H])N
-
別名
BCI 632
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)