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VU6024578

VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 -induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable[1].

Product Specifications

Product Name Alternative

BI02982816

UNSPSC

12352005

Target

MGluR

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Smiles

O=C(C1=CC(C2=CC=CO2)=CC=C1Cl)NCC3=CC(C4=CC=NN4C)=NN3C

Molecular Formula

C20H18ClN5O2

Molecular Weight

395.84

References & Citations

[1]Reed CW, et al., Discovery of VU6024578/BI02982816: An mGlu1 Positive Allosteric Modulator with Efficacy in Preclinical Antipsychotic and Cognition Models. J Med Chem. 2024 Dec 26;67 (24) :22291-22312.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

MGluR1

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