CID-16020046 is a selective GPR55 LPI receptor antagonist with IC50 of 015 M
CAS Number: 834903-43-4
Molecular Weight: 425.44
Chemical Name: 4-[4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1,4-dihydropyrrolo[3,4-d]pyrazol-5-yl]benzoic acid
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 85 mg/mL(199.79 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In 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 (CB1 or CB2). CID16020046 concentration dependently inhibited lysophosphatidylinositol (LPI)-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor κ of activated B cells (NF-κB) and serum response element, translocation of NFAT and NF-κB, and GPR55 internalization.
CID16020046 improves inflammation in models of intestinal inflammation and reduces proinflammatory cytokines. CID16020046 does not change the locomotor and anxiety behavior of healthy mice.
- Angela StanÄiÄ, et al. Neurogastroenterol Motil. 2015, 27(10): 1432-1445.
- Kargl J, et al. J Pharmacol Exp Ther. 2013, 346(1):54-66.
Products are for research use only. Not for human use.
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