HEP-50768 (HEP50768)

Chemical Structure : HEP-50768

Catalog No.: PC-26513Not For Human Use, Lab Use Only.

HEP-50768 is a potent and selective small-molecule inverse agonist of MRGPRX4 (hX4) with IC50 of 14 nM.

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Biological Activity

HEP-50768 is a potent and selective small-molecule inverse agonist of MRGPRX4 (hX4) with IC50 of 14 nM.
HEP-50768 with the (S)-configuration demonstrates significantly greater inhibitory activity than its (R)-enantiomer.
HEP-50768 exhibits minimal cross-reactivity with other itch-associated MRGPRX family members, shows only weak inhibition of MRGPRX1 (hX1) with an IC50 of 16 μM and MRGPRX2 (hX2) with an IC50 of 1.5 μM.
HEP-50768 also does not activate either hX1 or hX2.
HEP-50768 (5 or 10 mg kg, oral) alleviates DCA-3S-induced pruritus in an hX4-humanized rat model.

Physicochemical Properties

M.Wt	350.28
Formula	C16H10F4N4O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-5-(2-fluoro-3-(5-(trifluoromethyl)-2,3-dihydrobenzofuran-2-yl)phenyl)-1H-tetrazole

References

1. Jun Yang, et al. Nat Chem Biol. 2026 Apr 9. doi: 10.1038/s41589-026-02195-0.