Catalog Number
ACM834903434
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.
Synonyms
CID16020046; CID-16020046; CID 16020046
IUPAC Name
4-[4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1,4-dihydropyrrolo[3,4-d]pyrazol-5-yl]benzoic acid
Molecular Formula
C25H19N3O4
Canonical SMILES
O=C(O)C1=CC=C(N(C2=O)C(C3=CC=CC(O)=C3)C4=C2NN=C4C5=CC=C(C)C=C5)C=C1
InChI
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
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 70.58; H, 4.50; N, 9.88; O, 15.04
HS Tariff Code
2934.99.9001
In Vitro Activity
This study showed that AGEs dose dependently induced GPR55 expression in ATDC5 chondrocytes. The blockage of GPR55 by its newly discovered antagonist-CID16020046 mitigated AGEs- induced increase in cellular ROS and decrease in antioxidant NRF2.
Reference: Chem Biol Interact. 2020 Jul 1;325:109088. https://pubmed.ncbi.nlm.nih.gov/32360554/
In Vivo Activity
Further analysis of the component pain-related behaviours revealed that CID16020046 significantly reduced the duration of biting/licking/flinching behaviour (Pain 2) during the second phase of the formalin trial (Fig. 2C). Duration of paw elevation (Pain 1) during the second phase was also lower in CID16020046-treated rats but this effect did not reach statistical significance (Fig. 2B).
Reference: Neuroscience. 2020 Sep 1;443:19-29. https://pubmed.ncbi.nlm.nih.gov/32673629/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
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