5.06045
GPR55 Receptor Antagonist, CID16020046
别名:
GPR55 Receptor Antagonist, CID16020046, 4-[4-(3-Hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1H,4H-pyrrolo[3,4-c]pyrazol-5-yl]benzoic Acid
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关于此项目
经验公式（希尔记法）:
C25H19N3O4
化学文摘社编号:
分子量:
425.44
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
color
off-white
InChI
1S/C25H19N3O4/c1-14-5-7-15(8-6-14)21-20-22(27-26-21)24(30)28(18-11-9-16(10-12-18)25(31)32)23(20)17-3-2-4-19(29)13-17/h2-13,23,29H,1H3,(H,26,27)(H,31,32)
InChI key
VGUQVYZXABOXCX-UHFFFAOYSA-N
SMILES string
CC1=CC=C(C=C1)C2=NNC3=C2C(N(C3=O)C4=CC=C(C=C4)C(=O)O)C5=CC(=CC=C5)O
assay
≥99% (HPLC)
form
powder
potency
1 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
solubility
DMSO: 100 mg/mL
Quality Level
General description
A selective antagonist of G protein-coupled receptor 55 (GPR55) that blocks lipid L-a-lysophosphatidylinositol (LPI, Cat. No. 440153)-induced GPR55 activation (IC50 = 1 µM) and downstream effects in HEK293 cells. Also shown to block the agonistic effect of LPI on GPR55- expressing yeast cells (~10 µM). Inhibits LPI-induced Ca2+ mobilization and ERK1/2 phosphorylation in HEK-GPR55 and HEK-CB1 cells. However, it does not affect basal Ca2+ mobilization and ERK1/2 activity. Blocks the GPR55-mediated NFAT and NF-kB activation and their nuclear translocation in HEK-GPR55 cells. Diminishes LPI-induced wound healing in GPR55-expressing primary human lung microvascular endothelial cells and reverses LPI-inhibited platelet aggregation (~10 µM). Also reported to inhibit the activity of phosphodiesterases PDE3A and PDE4B (pIC50 = 5 and 4.8, respectively).
Biochem/physiol Actions
Primary Target
GPR55
GPR55
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kargl, J., et al, 2013. J. Pharmacol. Exp. Ther.346, 54.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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