529511-79-3
Chemical Structure
Beloranib hemioxalate
Synonym(s): ZGN-440 hemioxalate; ZGN-433 hemioxalate; CDK732 hemioxalate
- CAS No.: 529511-79-3
- Formula:C29H41NO6.1/2C2H2O4
- Molecular Weight:1089.32
SMILES: C[C@]1([C@H](O1)C/C=C(C)\C)[C@]2([H])[C@]3(CC[C@H]([C@H]2OC)OC(/C=C/C4=CC=C(C=C4)OCCN(C)C)=O)CO3.O=C(O)C(O)=O.[0.5]
Biological Activity:
Beloranib (ZGN-440; CKD-732 free base) hemioxalate is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib hemioxalate blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib hemioxalate significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib hemioxalate also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib hemioxalate can be used in research on obesity and hypothalamic obesity[1][2][3].
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Beloranib hemioxalate | Beloranib (ZGN-440; CKD-732 free base) hemioxalate is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib hemioxalate blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib hemioxalate significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib hemioxalate also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib hemioxalate can be used in research on obesity and hypothalamic obesity. |
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- [1]. Elfers CT, et al. Robust Reductions of Excess Weight and Hyperphagia by Beloranib in Rat Models of Genetic and Hypothalamic Obesity. Endocrinology. 2017;158(1):41-55. [Content Brief]
- [2]. Hughes TE, et al. Ascending dose-controlled trial of beloranib, a novel obesity treatment for safety, tolerability, and weight loss in obese women. Obesity (Silver Spring). 2013;21(9):1782-1788. [Content Brief]
- [3]. Huang HJ, et al. MetAP2 inhibition increases energy expenditure through direct action on brown adipocytes. J Biol Chem. 2019;294(24):9567-9575. [Content Brief]
Keywords
