VU 0357121 |
Catalog No.GC18087 |
VU 0357121 est un modulateur allostérique (PAM) mGlu5R positif et hautement sélectif avec une CE50 de 33 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 433967-28-3
Sample solution is provided at 25 µL, 10mM.
VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.IC50 Value: 33 nM(EC50)Target: mGluR5in vitro: VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. in vivo:
References:
[1]. Hammond, Alexis S.; Rodriguez, Alice L.; Townsend, Steven D. et al. Discovery of a Novel Chemical Class of mGlu5 Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chemical Neuroscience (2010), 1(10), 702-716.
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