A potent antagonist of NPY receptor Y5 (Kis = 1.3

MK-0557 – 10 mg

Brand:
Cayman
CAS:
328232-95-7
Storage:
-20
UN-No:
Non-Hazardous - /

MK-0557 is a potent antagonist of the neuropeptide Y (NPY) receptor Y5 (Kis = 1.3, 0.79, 0.74, and 1.4 nM for human, rhesus monkey, mouse, and rat receptors, respectively).{35182} It is >7,500-fold selective for Y5 over other receptors and lacks activity in a panel of 180 receptors, enzymes, and ion channels at concentrations up to 1 μM. MK-0557 increases intracellular calcium in CHO cells expressing the human Y5 receptor in a concentration-dependent manner. In vivo, MK-0557 (30 mg/kg) reduces body weight gain in wild-type and diet-induced obese mice. It also reduces retroperitoneal fat pad weight, epididymal and mesenteric fat pad weights, leptin levels, and food intake in lean mice fed a high-fat diet.  

 

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Description

A potent antagonist of NPY receptor Y5 (Kis = 1.3, 0.79, 0.74, and 1.4 nM for human, rhesus monkey, mouse, and rat receptors, respectively); >7,500-fold selective for Y5 over other NPY receptors and lacks activity in a panel of 180 receptors, enzymes, and ion channels at concentrations up to 1 μM; increases intracellular calcium in CHO cells expressing the human Y5 receptor in a concentration-dependent manner; reduces body weight gain in wild-type and diet-induced obese mice when administered at a dose of 30 mg/kg; reduces retroperitoneal fat pad weight, epididymal and mesenteric fat pad weights, leptin levels, and food intake in lean mice fed a high-fat diet

Formal name: trans-N-[1-(2-fluorophenyl)-1H-pyrazol-3-yl]-1′-oxo-spiro[cyclohexane-1,3′(1’H)-furo[3,4-c]pyridine]-4-carboxamide

Synonyms: 

Molecular weight: 406.4

CAS: 328232-95-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity||Research Area|Neuroscience|Behavioral Neuroscience|Food Intake||Research Area|Neuroscience|Neuroendocrinology

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