VUF16840 | ACKR3 inverse agonist | Probechem Biochemicals

Chemical Structure : VUF16840

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VUF16840 (VUF-16840)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	566.65
分子式	C31H36F2N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-((3S,4S)-1-cyclohexyl-3-((2-methoxyphenethyl)carbamoyl)piperidin-4-yl)-5-(2,4-difluorophenyl)isoxazole-3-carboxamide

参考文献

1. Bosma R, et al. Mol Pharmacol. 2025 Oct 26;107(12):100085.

VUF16840 (VUF-16840)

生物&药学活性

物理化学性质&存储条件

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VUF16840 (VUF-16840)

生物&药学活性

物理化学性质&存储条件

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