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JNJ-46778212

Chemical Structure : JNJ-46778212

CAS No.: 1363281-27-9

JNJ-46778212 (VU0409551;VU 0409551;JNJ 46778212;JNJ46778212)

Catalog No.: PC-60696Not For Human Use, Lab Use Only.

JNJ-46778212 (VU0409551) is a potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JNJ-46778212 (VU0409551) is a potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM.
JNJ-46778212 potentiates DHPG-induced long-term depression and induces calcium mobilization and ERK phosphorylation, does not potentiate mGlu5 modulation of NMDA receptor currents nor NMDA receptor-dependent long-term potentiation.
JNJ-46778212 demonstrates in vivo efficacy in multiple preclinical models o schizophrenia, coupled with good DMPK profile and acceptable therapeutic window.

Physicochemical Properties

M.Wt 352.365
Formula C20H17FN2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

100 mM in DMSO (35.2 mg/mL)

Chemical Name/SMILES

(4-fluorophenyl)(2-(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridin-5(4H)-yl)methanone

References

1. Conde-Ceide S, et al. ACS Med Chem Lett. 2015 May 20;6(6):716-20.

2. Zhou Y, et al. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3515-9.

3. Conde-Ceide S, et al. Bioorg Med Chem Lett. 2016 Jan 15;26(2):429-434.

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