A selective GPR55 inverse agonist
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CID-16020046

Item No. 15247

Technical Information
Formal Name
4-[4,6-dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]-benzoic acid
CAS Number
834903-43-4
Molecular Formula
C25H19N3O4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 25 mg/mlDMSO: 25 mg/ml
λmax
280 nm
SMILES
OC(C(C=C1)=CC=C1N2C(C3=CC=CC(O)=C3)C4=C(NN=C4C5=CC=C(C)C=C5)C2=O)=O
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CID-16020046 is a GPR55 inverse agonist that antagonizes GPR55 constitutive activity with an IC50 value of 15 μM.1 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.1 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.1 This compound has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kargl, J., Brown, A.J., Andersen, L., et alA selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J. Pharmacol. Exp. Ther. 346(1), 54-66 (2013).