VU0400195
VU0400195 (ML182) is a oral active and allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4) with the EC50 of 291 nM. VU0400195 can be used for study of antiparkinsonian animal model.
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: 1309434-83-0
- 分子式: C21H16ClN3O3
- 分子量:393.82
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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
IC50 & Target
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hmGluR4a 291 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
291 nM
Compound: 15f, VU0400195, ML182, diastereomeric mixture
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Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay
Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay
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[PMID: 21966889] |
| HEK293 | EC50 |
1.7 μM
Compound: 15f, VU0400195, ML182, diastereomeric mixture
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Positive allosteric modulator activity at rat mGlu5 receptor expressed in human HEK293 at 10 uM by calcium mobilization assay
Positive allosteric modulator activity at rat mGlu5 receptor expressed in human HEK293 at 10 uM by calcium mobilization assay
|
[PMID: 21966889] |
化学情報
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CAS 番号 1309434-83-0
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分子量 393.82
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分子式 C21H16ClN3O3
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SMILES
O=C(C1=NC=CC=C1)NC2=CC=C(C(Cl)=C2)N3C([C@@]4([C@@]5([H])C[C@@]([H])([C@]4([H])C3=O)C=C5)[H])=O
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別名
ML182
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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.
プロトコル
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
純度とドキュメンテーション
参考文献
[1]. Jones CK, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model. J Med Chem. 2011 Nov 10;54(21):7639-47. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)