2011754-00-8
Chemical Structure
BDM44768
- CAS No.: 2011754-00-8
- Formula:C24H22FN5O3
- Molecular Weight:447.46
IUPAC Name: (R)-4-fluoro-N-((1-(4-(hydroxyamino)-1-(naphthalen-2-yl)-4-oxobutan-2-yl)-1H-1,2,3-triazol-4-yl)methyl)benzamide
InChIKey: RASCFMYPAZDCKQ-JOCHJYFZSA-N
SMILES: ONC(C[C@H](N1C=C(N=N1)CNC(C2=CC=C(C=C2)F)=O)CC3=CC4=C(C=CC=C4)C=C3)=O
Biological Activity: BDM44768 is an insulin-degrading enzyme (IDE) inhibitor (human IC50 = 0.06 μM; Ki = 60 nM). BDM44768 impairs D-Glucose (HY-B0389) tolerance, enhances Insulin (HY-P0035) signaling, and increases Amyloid-β concentration in an IDE-dependent manner by chelating the catalytic zinc, stabilizing the closed conformation, and binding the substrate/catalytic cleft. BDM44768 can be used in research on diabetes and metabolic dysfunction-associated steatotic liver disease (MASLD)[1][2][3][4][5][6].
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BDM44768 | BDM44768 is an insulin-degrading enzyme (IDE) inhibitor (human IC50 = 0.06 μM; Ki = 60 nM). BDM44768 impairs D-Glucose (HY-B0389) tolerance, enhances Insulin (HY-P0035) signaling, and increases Amyloid-β concentration in an IDE-dependent manner by chelating the catalytic zinc, stabilizing the closed conformation, and binding the substrate/catalytic cleft. BDM44768 can be used in research on diabetes and metabolic dysfunction-associated steatotic liver disease (MASLD). | |||||||||||||||||||||
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References
- [1]. Deprez-Poulain R, et al. Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice. Nature communications. 2015 Sep 23;6:8250. [Content Brief]
- [2]. González-Casimiro CM, et al. Modulation of Insulin Sensitivity by Insulin-Degrading Enzyme. Biomedicines. 2021 Jan 17;9(1):86.
- [3]. Leissring MA, et al. Targeting Insulin-Degrading Enzyme in Insulin Clearance. International journal of molecular sciences. 2021 Feb 24;22(5):2235.
- [4]. Andres M, et al. Insulin-degrading enzyme inhibition increases the unfolded protein response and favours lipid accumulation in the liver. British journal of pharmacology. 2024 Oct;181(19):3610-3626. [Content Brief]
- [5]. Parvatkar PT, et al. Biocompatible reactions: Advances in kinetic target-guided synthesis. Trends in Chemistry. 2023 Sep 1;5(9):657-71.
- [6]. Leroux F, et al. Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening. European journal of medicinal chemistry. 2019 Oct 01;179:557-566.
