ML192

Names

[ Name ]:
ML192

[Synonym ]:
2-furanyl-[4-(2-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-4-yl)-1-piperazinyl]methanone
Furan-2-yl-[4-(2-methyl-5,6,7,8-tetrahydro-benzo[4,5]thieno[2,3-d]pyrimidin-4-yl)-piperazin-1-yl]-methanone
ML-192
2-Furyl[4-(2-methyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1-piperazinyl]methanone
Methanone, 2-furanyl[4-(5,6,7,8-tetrahydro-2-methyl[1]benzothieno[2,3-d]pyrimidin-4-yl)-1-piperazinyl]-

Biological Activity

[Description]:

ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> GPR55

Signaling Pathways >> MAPK/ERK Pathway >> ERK

Signaling Pathways >> TGF-beta/Smad >> PKC

Signaling Pathways >> Stem Cell/Wnt >> ERK

[Target]

ERK2

ERK1

PKCβII

[In Vitro]

ML192 抑制 10 μM L-α 溶血磷脂酰肌醇 (LPI) 或 1 μM ML186 诱导的 β-arrestin 转运，IC50 值分别为0.70μM、0.29 µM[1]。 ML192 显著抑制表达 GPRSS 的 U2OS 细胞中 ERK1/2 的磷酸化[1]。 ML192 (0, 10, 30 和 100 µM) 减弱了野生型 GPR55 受体细胞中的 PKCβII 易位[1]。

[References]

[1]. Kotsikorou E, et al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2013 Dec 31;52(52):9456-69.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₂₀H₂₂N₄O₂S

[ Molecular Weight ]:
382.479

[ Exact Mass ]:
382.146332

[ LogP ]:
3.07

[ Index of Refraction ]:
1.664

[ Storage condition ]:
2-8°C

Related Compounds

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