MK-5046_product_DataBase

Bioactivity

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].

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)

Invitro

MK-5046 对人、小鼠、大鼠、狗和猕猴 BRS3 的 IC50 值分别为 28、5.4、1.2、6.5 和 50 nM[2]。MK-5046 对人、小鼠、大鼠、狗和猕猴 BRS3 的 Ki 值分别为 3.4、1.6、0.6、9.9 和 2.4 nM[2]。MK-5046 对人、小鼠、大鼠、狗和猕猴 BRS3 的 EC50 值分别为 14、21、2.2、1.6 和 6.9 nM [2]。MK-5046 抑制兔钙离子通道 diltiazem (DLZ) 位点，IC50 值为 1.9 μM[2]。

In Vivo

MK-5046 (3, 10 和 30 mg/kg；口服，一次) 抑制食物摄入，并提高饮食诱导肥胖 (DIO) 小鼠的静息代谢率 (MR) 和体温[1]。MK-5046 (5，25 和 50 mg/kg；皮下注射，每天一次，连续 14 天) 显著降低 DIO 小鼠的体重和食物摄入量[1]。 Animal Model:

Name

MK-5046

CAS

1022152-70-0

Formula

C20H18F6N4O

Molar Mass

444.37

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Guan XM, et al. Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther. 2011 Feb;336(2):356-364. [2]. Sebhat IK, et al. Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett. 2010 Oct 18;2(1):43-47. [3]. Ramos-Alvarez I, et al. The Nonpeptide Agonist MK-5046 Functions As an Allosteric Agonist for the Bombesin Receptor Subtype-3. J Pharmacol Exp Ther. 2022 Aug;382(2):66-78.

PeptideDB

MK-5046

CAS: 1022152-70-0 F: C20H18F6N4O W: 444.37