CID 16020046

SKU: orb1221742

Description

CID16020046 is a selective GPR55 inverse agonist. CID16020046 is a G protein-coupled receptor that is weakly activated by some cannabinoids at nM concentrations. CID16020046 has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.(In Vitro):CID 16020046 has weak activities close for inhibition of the acetylcholinesterase (pIC50=4.4), antagonism of the m-opioid receptor (pIC50=4.6), and blockade of KCNH2, the hERG channel (pIC50=4.6) 6 in human embryonic kidney (HEK)-G protein–coupled receptor 55 (GPR55) cells.CID 16020046 (2.5 μM; for ≥25 minutes) significantly inhibits the lysophosphatidylinositol (LPI; 2.5 μM) induced ERK1/2 phosphorylation. CID 16020046 alone fails to induce intracellular Ca2+ release in HEK-GPR55, HEKCB1 cells and shows no ERK1/2 phosphorylation.Pretreatment with CID16020046 (0.01, 0.1, 1, 10 μM) leads to a concentration-dependent decrease in GPR55-mediated NFAT activation, NF-kB activation, and SRE induction in response to 1 μM LPI or GSK319197A in HEKGPR55 and HEK-CB1 cells.CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation.Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls.

Key Properties

• CAS Number: 834903-43-4
• MW: 425.44
• Purity: >98% (HPLC)
• Formula: C₂₅H₁₉N₃O₄
• SMILES: CC1=CC=C(C=C1)C2=NNC3=C2C(N(C3=O)C4=CC=C(C=C4)C(=O)O)C5=CC(=CC=C5)O
• Target: GPR55
• Solubility: DMSO : ≥ 28 mg/mL; 65.81 mM

Bioactivity

• In Vitro:
  Western blot analysis. Cell line: HEK-CB1 and HEK-CB2 cells. Concentration: 2.5 μM Incubation time: For ≥25 minutes. Result: Significantly inhibited the LPI (2.5 μM) induced ERK1/2 phosphorylation. Treatment alone showed no ERK1/2 phosphorylation and did not alter WIN55, 212-2 (2.5 μM) induced ERK1/2 phosphorylation in HEK-CB1 and HEK-CB2 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CID16020046 | CID-16020046

Quick Database Links

Gene Symbol

GPR55