CID 16020046

Modify Date: 2024-01-14 21:21:00

CID 16020046 Structure
CID 16020046 structure
Common Name CID 16020046
CAS Number 834903-43-4 Molecular Weight 425.43600
Density N/A Boiling Point N/A
Molecular Formula C25H19N3O4 Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of CID 16020046


CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM.IC50 value: 0.15 uM [1]Target: GPR55 antagonistIn yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney(HEK293) cells stably expressing human GPR55, the compound behaved as an antagonist on LPI-mediated Ca2+ release and extracellular signal-regulated kinases activation, but not in HEK293 cells expressing cannabinoid receptor 1 or 2.CID16020046 concentration dependently inhibited LPI-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor k of activated B cells (NF-kB) and serum response element, translocation of NFAT and NF-kB, and GPR55 internalization. It reduced LPI-induced wound healing in primary human lung microvascular endothelial cells and reversed LPI-inhibited platelet aggregation.

 Names

Name Benzoic acid, 4-[4,6-dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]
Synonym More Synonyms

 CID 16020046 Biological Activity

Description CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM.IC50 value: 0.15 uM [1]Target: GPR55 antagonistIn yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney(HEK293) cells stably expressing human GPR55, the compound behaved as an antagonist on LPI-mediated Ca2+ release and extracellular signal-regulated kinases activation, but not in HEK293 cells expressing cannabinoid receptor 1 or 2.CID16020046 concentration dependently inhibited LPI-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor k of activated B cells (NF-kB) and serum response element, translocation of NFAT and NF-kB, and GPR55 internalization. It reduced LPI-induced wound healing in primary human lung microvascular endothelial cells and reversed LPI-inhibited platelet aggregation.
Related Catalog
References

[1]. Kargl J, et al. A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther. 2013 Jul;346(1):54-66.

 Chemical & Physical Properties

Molecular Formula C25H19N3O4
Molecular Weight 425.43600
Exact Mass 425.13800
PSA 106.52000
LogP 4.60370
Storage condition -20℃

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319
Precautionary Statements P305 + P351 + P338
RIDADR NONH for all modes of transport

 Synonyms

cid 16020046
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