VU 0409551

Pricing Availability Delivery Time Qty
Cat.No. 5693 - VU 0409551 | C20H17FN2O3 | CAS No. 1363281-27-9
Description: Selective mGlu5 positive allosteric modulator; 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% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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 Gαq. 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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1363281-27-9
PubChem ID 56846694
InChI Key QUZLMKNNIUSREV-UHFFFAOYSA-N
Smiles O=C(C1=CC=C(F)C=C1)N(C2)CCC3=C2OC(COC4=CC=CC=C4)=N3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.24 100
ethanol 17.62 50

Preparing Stock Solutions

The following data is based on the product molecular weight 352.36. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.84 mL 14.19 mL 28.38 mL
5 mM 0.57 mL 2.84 mL 5.68 mL
10 mM 0.28 mL 1.42 mL 2.84 mL
50 mM 0.06 mL 0.28 mL 0.57 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

Rook et al (2015) Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents. Neuron 86 1029 PMID: 25937172

Conde-Ceide et al (2015) Discovery of VU0409551/JNJ-46778212: An mGlu5 positive allosteric modulator clinical candidate targeting schizophrenia. ACS Med.Chem.Lett. 6 716 PMID: 26157544


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Keywords: JNJ46778212 VU0409551 metabotropic glutamate receptors mGlu5 positive allosteric modulators modulates PAMs JNJ 46778212 Glutamate (Metabotropic) Group I Receptors

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