VU6005649

Research use only, not for human use.

VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).

VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).(In Vitro):VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively). VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50.(In Vivo):In wild-type mice, VU6005649 shows modest but significant pro-cognitive effects on associative learning and the first example of the efficacy of a mGlu7/8 positive allosteric modulator (PAM) in this model.

VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively. VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50.

When VU6005649 (compound 9f) is dosed at 30 mg/kg IP in 10% Tween 80/H2O (0.75 mg/kg. s.c. amphetamine), no efficacy is observed in this assay. VU6005649 shows modest but significant pro-cognitive effects on associative learning in wild-type mice and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model.

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Neuroscience

GluR

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2137047-43-7

357.284

C16H12F5N3O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (139.95 mM)

COc1ccc(-c2c(C)nn3c(cc(C)nc23)C(F)(F)F)c(F)c1F

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(-20℃)

With Ice Pack

≥ 2 years