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DF3016A

Chemical Structure : DF3016A

CAS No.: 2351103-44-9

DF3016A (DF 3016A)

Catalog No.: PC-38338Not For Human Use, Lab Use Only.

DF3016A (DF 3016A) is a potent and selective C5aR inhibitor with IC50 of 50 nM (C5a-induced human PMN migration and IC50 of 45 and 37 nM against rat and mouse C5aR, respectively.

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    Biological Activity

    DF3016A (DF 3016A) is a potent and selective C5aR inhibitor with IC50 of 50 nM (C5a-induced human PMN migration and IC50 of 45 and 37 nM against rat and mouse C5aR, respectively.
    DF3016A exhibited a high degree of selectivity with no effect on PMN migration induced by other leukocyte activators such as CXCL8, CXCL1, CCL3, fMLP, CXCL12, and on LPS-induced PGE2 accumulation at 10 uM.
    DF3016A protects neuronal viability by restoring intracellular calcium levels, thus opposing the increase in pro-inflammatory cytokine levels and miR-181 expression in rat model of neuroinflammatory injury.
    DF3016A also inhibits osteoclast degradation activity through inhibition of C5aR signal transduction and transcription.

    Physicochemical Properties

    M.Wt 362.31
    Formula C13H10F3N6NaS
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 1 Month
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    sodium (R)-5-(1-(4-((4-(trifluoromethyl)thiazol-2-yl)amino)phenyl)ethyl)tetrazol-1-ide

    References

    1. Rosa D'Angelo, et al. Biomed Pharmacother. 2020 Mar;123:109764.

    2. Laura Brandolini, et al. Neurotox Res. 2019 Jul;36(1):163-174.

    3. Grannonico M, et al. Brain Res. 2020 Dec 1;1748:147057.

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