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CID16020046 (CAS 834903-43-4) LS-H116

GPR55 antagonist
LS-H116-1 / 1 mg / $185
LS-H116-5 / 5 mg / $215
LS-H116-10 / 10 mg / $265
LS-H116-25 / 25 mg / $385
USA Shipment Only
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Description: GPR55 is a G protein-coupled receptor (GPCR) that is weakly activated by some cannabinoids (CBs) at nM concentrations but displays a 5- to 10-fold greater stimulation in response to 1 µM lysophosphatidylinositol (LPI). CID16020046 is a GPR55 inverse agonist that antagonizes GPR55 constitutive activity with an IC50 value of 15 µM. It inhibits GPR55-mediated ERK1/2 phosphorylation, LPI-induced Ca2+ signaling (IC50 = 0.21 µM in HEK-GPR55 cells), and GPR55-mediated transcription factor activation. It does not affect ERK1/2 phosphorylation or transcription factor activation in CB receptor expressing cells and demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptors. This compound has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation. H116_ChemicalStructureImage.png
4-[4,6-dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]-benzoic acid
biochemical, chemical, antagonist
A crystalline solid
Shipped at 4°C, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: GPR55 related products

Usage Information

CID16020046 is supplied as a crystalline solid. A stock solution may be made by dissolving the CID16020046 in the solvent of choice. CID16020046 is soluble in organic solvents such as DMSO and dimethyl formamide, which should be purged with an inert gas. The solubility of CID16020046 in these solvents is approximately 0.1 and 0.2 mg/ml, respectively. CID16020046 is sparingly soluble in aqueous solutions. To enhance aqueous solubility, dilute the organic solvent solution into aqueous buffers or isotonic saline. If performing biological experiments, ensure the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day.

  1. Ryberg, E., Larsson, N., Sjögren, S., et al. The orphan receptor GPR55 is a novel cannabinoid receptor. Br. J. Pharmacol. 152, 1092-1101 (2007).
  2. Oka, S., Nakajima, K., Yamashita, A., et al. Identification of GPR55 as a lysophosphatidylinositol receptor. Biochem. Biophys. Res. Commun. 362, 928-934 (2007).
  3. Kargl, J., Brown, A.J., Andersen, L., et al. A selective antagonist reveals a potential role of G proteincoupled receptor 55 in platelet and endothelial cell function. J. Pharmacol. Exp. Ther. 346, 54-66 (2013).

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