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Catalog: | HY-16697 |
Brand: | MCE |
CAS: | 834903-43-4 |
MDL | MFCD06196075 |
---|---|
Molecular Weight | 425.44 |
Molecular Formula | C25H19N3O4 |
SMILES | O=C(O)C1=CC=C(N(C2C3=CC=CC(O)=C3)C(C4=C2C(C5=CC=C(C)C=C5)=NN4)=O)C=C1 |
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC 50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function [1] .
CID 16020046 has weak activities close for inhibition of the acetylcholinesterase (pIC
50
=4.4), antagonism of the m-opioid receptor (pIC
50
=4.6), and blockade of KCNH2, the hERG channel (pIC
50
=4.6) 6 in human embryonic kidney (HEK)-G protein–coupled receptor 55 (GPR55) cells
[1]
.
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 Ca
2+
release in HEK-GPR55, HEKCB1 cells and shows no ERK1/2 phosphorylation
[1]
.
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
[1]
.
CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation
[1]
.
Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
Cell Line: | HEK-CB1 and HEK-CB2 cells [1] |
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. |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 100 mg/mL ( 235.05 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.3505 mL | 11.7525 mL | 23.5051 mL |
5 mM | 0.4701 mL | 2.3505 mL | 4.7010 mL |
10 mM | 0.2351 mL | 1.1753 mL | 2.3505 mL |
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