VU0650786

• CAT Number: I019278
• CAS Number: 1809085-30-0
• Purity: ≥95%
• Synonyms: (7R)-2-[(5-chloropyridin-2-yl)oxymethyl]-5-(2-fluoropyridin-3-yl)-7-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-4-one
• InChI: InChI=1S/C18H15ClFN5O2/c1-11-9-24(14-3-2-6-21-17(14)20)18(26)15-7-13(23-25(11)15)10-27-16-5-4-12(19)8-22-16/h2-8,11H,9-10H2,1H3/t11-/m1/s1
• InChIKey: RXRVCJFGSOVYLG-LLVKDONJSA-N
• SMILES: CC1CN(C(=O)C2=CC(=NN12)COC3=NC=C(C=C3)Cl)C4=C(N=CC=C4)F

VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents[1].
VU0650786 (VU786) (i.p., 30 mg/kg) increases the proportion of c-Fos-positive cells by approximately 4-fold, enhances synaptic strength in cone cell subpopulations, weakens thalamocortical long-term depression (LTD), and reduces passive coping in acute models of antidepressant-like activity in inducible cFos-EGFP mice[2].
The pharmacokinetic parameters of VU0650786 (compound 106) in rats[1].

Parameters
IV (0.2 mg/kg)

t1/2 (min)
42

CL plasma (mL/min/kg)
37

VSS (L/kg)
1.6