MK-5046

MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC₅₀ and an EC₅₀ value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity^[1][2][3]. IC50 & Target:IC50: 28 nM (human BRS3), 5.4 nM (mouse BRS3), 1.2 nM (rat BRS3), 6.5 nM (dog BRS3), 50 nM (rhesus BRS3)^[2] In Vitro:MK-5046 shows IC₅₀ values of 28, 5.4, 1.2, 6.5 and 50 nM for BRS3 of human, mouse, rat, dog and rhesus, respectively^[2].
MK-5046 exhibits K_i values of 3.4, 1.6, 0.6, 9.9 and 2.4 nM for BRS3 of human, mouse, rat, dog and rhesus, respectively^[2].
MK-5046 shows EC₅₀ values of 14, 21, 2.2, 1.6 and 6.9 nM for BRS3 of human, mouse, rat, dog and rhesus, respectively^[2].
MK-5046 inhibits diltiazem (DLZ) site of the rabbit calcium ion channel with an IC₅₀ value of 1.9 μM^[2]. In Vivo:MK-5046 (3, 10 and 30 mg/kg; oral administration for once) inhibits food intake, and increases resting metabolic rate (MR) and body temperature in DIO mice^[1].
MK-5046 (5, 25 and 50 mg/kg; s.c. once daily for 14 days) significantly reduces body weight and food intake in DIO mice^[1].