>>Signaling Pathways>> GPCR/G protein>> mGluR >>VU 0357121

VU 0357121

Catalog No.GC18087

VU 0357121은 33nM의 EC50을 갖는 양성 및 고선택성 mGlu5R 알로스테릭 조절제(PAM)입니다.

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VU 0357121 Chemical Structure

Cas No.: 433967-28-3

Size 가격 재고 수량
10mg
US$57.00
재고 있음
25mg
US$117.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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