Chemical Structure : VUF16840
CAS No.:
2178050-87-6
VUF16840
(VUF-16840)
Catalog No.: PC-25858Not For Human Use, Lab Use Only.
VUF16840 is a potent and selective small-molecule inverse agonist of ACKR3 (CXCR7), displaces CXCL12-A647 binding to NLuc-hACKR3 with IC50 of 7 nM, suppresses constitutive signaling of ACKR3.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
VUF16840 is a potent and selective small-molecule inverse agonist of ACKR3 (CXCR7), displaces CXCL12-A647 binding to NLuc-hACKR3 with IC50 of 7 nM, suppresses constitutive signaling of ACKR3.
VUF16840 fully displaced [3H]VUF15485 binding from hACKR3 with IC50 of 0.7 nM.
VUF16840 inhibits constitutive as well as agonist induced β-arrestin2 recruitment to ACKR3.
VUF16840 only modulates ACKR3 and CCR3 at pharmacologically relevant concentrations, demonstrates high selectivity for ACKR3 over other chemokine receptors.
VUF16840 inhibits constitutive ACKR3 signaling and trafficking events.
VUF16840 blocks CXCL12 uptake in ACKR3 expressing endothelial cells.
Physicochemical Properties
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M.Wt
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566.65
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Formula
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C31H36F2N4O4
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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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N-((3S,4S)-1-cyclohexyl-3-((2-methoxyphenethyl)carbamoyl)piperidin-4-yl)-5-(2,4-difluorophenyl)isoxazole-3-carboxamide
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References
1. Bosma R, et al. Mol Pharmacol. 2025 Oct 26;107(12):100085.
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