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JNJ-46778212

Chemical Structure : JNJ-46778212

CAS No.: 1363281-27-9

JNJ-46778212 (VU0409551, 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 of 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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