Ro4491533
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
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: 579482-31-8
- 分子式: C24H20F3N3O
- 分子量:423.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
<0.01 μM
Compound: 7am
|
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
| CHO | IC50 |
<0.01 μM
Compound: 7am
|
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
| CHO | IC50 |
0.003 μM
Compound: 7am
|
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
|
[PMID: 20971004] |
| CHO | IC50 |
0.014 μM
Compound: 7am
|
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
化学情報
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CAS 番号 579482-31-8
-
分子量 423.43
-
分子式 C24H20F3N3O
-
SMILES
O=C1NC2=CC(C(F)(F)F)=C(C=C2N=C(C1)C3=CC=CC(C4=CC(C)=NC(C)=C4)=C3)C
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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)