TC-FPR 43 - CAS 903895-98-7
Category: Inhibitor
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Molecular Formula:
C20H21ClN4O2
Molecular Weight:
384.86
COA:
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Targets:
Others
Description:
TC-FPR 43 is a potent formyl peptide receptor 2 (FPR2) agonist (EC50 = 44 nM) that inhibits fMLP- and IL-8-induced neutrophil migration and induces calcium mobilization. TC-FPR 43 was shown to suppress inflammation in a mouse model of acute inflammation. It also acts as an ALX agonist.
Brife Description:
FPR2 agonist
Purity:
≥98% by HPLC
Synonyms:
TCFPR43; TC FPR 43; TC-FPR-43; N-(4-Chlorophenyl)-N-[2,3-dihydro-1-methyl-5-(1-methylethyl)-3-oxo-2-phenyl-1H-pyrazol-4-yl]-urea; Pyrazolone, 1
MSDS:
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InChIKey:
PAEBEUZTAPIOIO-UHFFFAOYSA-N
InChI:
InChI=1S/C20H21ClN4O2/c1-13(2)18-17(23-20(27)22-15-11-9-14(21)10-12-15)19(26)25(24(18)3)16-7-5-4-6-8-16/h4-13H,1-3H3,(H2,22,23,27)
Canonical SMILES:
CC(C)C1=C(C(=O)N(N1C)C2=CC=CC=C2)NC(=O)NC3=CC=C(C=C3)Cl
1.Formyl peptide receptor activation inhibits the expansion of effector T cells and synovial fibroblasts and attenuates joint injury in models of rheumatoid arthritis.
Odobasic D;Jia Y;Kao W;Fan H;Wei X;Gu R;Ngo D;Kitching AR;Holdsworth SR;Morand EF;Yang YH Int Immunopharmacol. 2018 Aug;61:140-149. doi: 10.1016/j.intimp.2018.05.028. Epub 2018 Jun 4.
The effects of formyl peptide receptors (FPRs) on effector T cells and inflammation-causing tissue-resident cells are not well known. Here, we explored the effect of FPR activation on efferent T cell responses in models of rheumatoid arthritis (RA) and on the expansion of fibroblast-like synoviocytes (FLS). Compound 43 (Cpd43; FPR1/2 agonist) was administered to mice with collagen-induced arthritis (CIA) or antigen-induced arthritis (AIA) after disease onset. Joint inflammation/damage and immunity were assessed. FLS were cultured with Cpd43 to test its effects on cell apoptosis and proliferation. To explore the effects of endogenous FPR2 ligands on FLS proliferation, FLS FPR2 was blocked or Annexin A1 (AnxA1) expression silenced. Cpd43 reduced arthritis severity in both models. In CIA, Cpd43 decreased CD4 T cell proliferation and survival and increased the production of the protective cytokine, IFNγ, in lymph nodes. In AIA, Cpd43 increased CD4 apoptosis and production of the anti-inflammatory IL-4, while augmenting the proportion of splenic regulatory T cells and their expression of IL-2Rα. In both models, Cpd43 increased CD4 IL-17A production, without affecting humoral immunity. FPR2 inhibitors reversed Cpd43-mediated effects on AIA and T cell immunity.
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CAS 903895-98-7 TC-FPR 43

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