VU 0409551

Catalog #: 5693 Datasheet / COA / SDS

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VU 0409551 | CAS No. 1363281-27-9 | Group I mGluR Modulators

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Description: Selective positive allosteric modulator of mGlu5 receptors; brain penetrant and orally bioavailable

Alternative Names: JNJ 46778212

Chemical Name: [6,7-Dihydro-2-(phenoxymethyl)oxazolo[5,4-c]pyridin-5(4H)-yl](fluorophenyl)methanone

Purity: ≥98%

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Biological Activity

VU 0409551 is a selective mGlu₅ positive allosteric modulator (EC₅₀ = 260 nM). Selective for mGlu₅ over other mGluR subtypes, as well as 66 other receptors and ion channels. Selectively potentiates mGlu₅ signaling via G_αq. Exhibits wake-promoting, antipsychotic-like and cognition-enhancing effects in animal models. Brain penetrant and orally available.

Technical Data

M.Wt:

352.36

Formula:

C₂₀H₁₇FN₂O₃

Solubility:

Soluble to 100 mM in DMSO and to 50 mM in ethanol

Purity:

≥98%

Storage:

Store at +4°C

CAS No:

1363281-27-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

Role of mGlu5 receptors and inhibitory neurotransmission in M1 dependent muscarinic LTD in the prefrontal cortex: implications in Schizophrenia.
Ghoshal et al.
ACS Chem.Neurosci., 2017;8:2254
Biased mGlu₅-positive allosteric modulators provide in vivo efficacy without potentiating mGlu₅ modulation of NMDAR currents.
Rook et al.
Neuron, 2015;86:1029
Discovery of VU0409551/JNJ-46778212: An mGlu₅ positive allosteric modulator clinical candidate targeting schizophrenia.
Conde-Ceide et al.
ACS Med.Chem.Lett., 2015;6:716

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