New GPR Modulators

Catalog No.	Product Name	Information
S2950	SBI-553	SBI-553 is a β-arrestin–biased, brain-penetrant positive allosteric modulator (PAM) of the neurotensin receptor 1 (NTSR1/NTR1), with an EC50 of 0.34 μM in cellular assays.
E6710	MKP10241	MKP10241 is a potent, orally active agonist of GPR119 that elevates cAMP levels in a GPR119‑expressing cell line with an EC50 ≈ 3.7 nM. MKP10241 reduces blood glucose and HbA1c in acute and chronic diabetic mouse models and shows excellent preclinical efficacy in rodent models of obesity and MASH.
E6677	CATPB	CATPB is an antagonist of FFA2R that inhibits the transient rise in intracellular Ca²⁺ induced in neutrophils by acetate or the synthetic FFAR2 agonist Cmp1, thereby blocking downstream FFAR2‑dependent activation responses, including NADPH oxidase–derived superoxide production.
E6776	AP-503	AP‑503 is a selective agonist of GPR133/ADGRD1 with an EC50 of 1.21 nM. It exhibits the potential to be used in research on the prevention of muscle‑related diseases and vestibular dysfunction.
E6738	BCFTP	BCFTP is a potent, orally active, selective positive allosteric modulator (PAM) of human MrgprX1 that enhances endogenous ligand signaling to inhibit spinal C-fibre nociceptive transmission, thereby relieving heat hyperalgesia and spontaneous pain in neuropathic models without itch or tolerance.
≡ All GPR Modulators