Chemical Structure : PF-07054894
CAS No.:
2413693-96-4
PF-07054894
(PF 07054894)
Catalog No.: PC-20761Not For Human Use, Lab Use Only.
PF-07054894 is a potent, functionally selective CCR6 antagonist, blocks in vitro CCL20- dependent human T cell chemotaxis with IC50 of 5.7 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PF-07054894 is a potent, functionally selective CCR6 antagonist, blocks in vitro CCL20- dependent human T cell chemotaxis with IC50 of 5.7 nM.
PF-07054894 dispays negligible activity (<12% over basal activity) in an assay panel of 168 G protein-coupled receptors, with more than 30% inhibition of agonist-dependent activity on only 3 receptors: CCR6, CCR7, and CXCR2.
PF-07054894 displays >50- and 150-fold functional selectivity relative to CCR7 and CXCR2.
PF-07054894 increased the frequency of CCR6+ peripheral blood T cells suggesting that blockade of CCR6 inhibited homeostatic migration of T cells from blood to tissues of naïve cynomolgus monkeys.
PF-07054894 caused an increase in cell surface CCR6 in mouse and monkey B cells which was recapitulated in mouse splenocytes in vitro.
Physicochemical Properties
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M.Wt
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466.54
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Formula
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C24H30N6O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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O=C(N(C)C)C1=NC=CC(NC2=C(N[C@@H](C3=NN(C)C=C3C)C4(C)CCCC4)C(C2=O)=O)=C1O
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References
1. Wei Li, et al. J Pharmacol Exp Ther. 2023 May 4;JPET-AR-2022-001452.
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