BMS-955829
BMS-955829 is an orally active and selective mGluR5 positive allosteric modulator with an EC50 of 2.6 nM. BMS-955829 has no intrinsic agonist activity and a low glutamate fold shift (2.4). BMS-955829 can effectively improve cognitive and executive function deficits in rodents. BMS-955829 can be used in the research of cognitive impairment diseases such as schizophrenia.
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: 1375751-08-8
- 分子式: C22H14F2N2O2
- 分子量:376.36
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>30 μM
Compound: 4; BMS-955829
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Agonist activity at human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as induction of Ca2+ release by calcium 4 dye based FLIPR assay
Agonist activity at human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as induction of Ca2+ release by calcium 4 dye based FLIPR assay
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[PMID: 26985317] |
| HEK293 | EC50 |
>3000 nM
Compound: 12; BMS-955829
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Agonist activity at human mGluR5A transfected in HEK293 cells assessed as induction of calcium release by FLIPR assay
Agonist activity at human mGluR5A transfected in HEK293 cells assessed as induction of calcium release by FLIPR assay
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[PMID: 27496211] |
| HEK293 | EC50 |
2.6 nM
Compound: 12; BMS-955829
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Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay
Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay
|
[PMID: 27496211] |
| HEK293 | EC50 |
2.6 nM
Compound: 4; BMS-955829
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Positive allosteric modulation of human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as potentiation of L-glutamate-induced Ca2+ signal incubated for 60 mins by calcium 4 dye based FLIPR assay
Positive allosteric modulation of human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as potentiation of L-glutamate-induced Ca2+ signal incubated for 60 mins by calcium 4 dye based FLIPR assay
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[PMID: 26985317] |
| HEK293 | IC50 |
3 nM
Compound: BMS-955829
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Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis
Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis
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[PMID: 27994742] |
化学情報
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CAS 番号 1375751-08-8
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分子量 376.36
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分子式 C22H14F2N2O2
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SMILES
O=C1O[C@H](C2=CC(F)=CC=C2F)[C@@H](C3=CC(C#CC4=CC=CC=C4)=CN=C3)N1
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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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BMS-955829 関連分類
HY-120641 関連分類
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