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.
For research use only. We do not sell to patients.
- CAS No.: 1309434-83-0
- Formula: C21H16ClN3O3
- Molecular Weight:393.82
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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
|
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] |
Chemical Information
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CAS No. 1309434-83-0
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Molecular Weight 393.82
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Formula 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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Synonyms
ML182
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)