145253-48-1
Chemical Structure
RB104
- CAS No.: 145253-48-1
- Formula:C21H23IN2O6
- Molecular Weight:526.33
IUPAC Name: 2-(4-hydroxy-3-iodobenzyl)-4-((4-(hydroxyamino)-4-oxo-1-phenylbutan-2-yl)amino)-4-oxobutanoic acid
InChIKey: SPYDLFCJSOZVCF-UHFFFAOYSA-N
SMILES: O=C(O)C(CC(=O)NC(CC(=O)NO)CC=1C=CC=CC1)CC2=CC=C(O)C(I)=C2
Biological Activity: RB104 is a highly selective neutral endopeptidase (NEP) inhibitor that exhibits extremely high affinity for Aplysia californica apNEP (Kd=0.16-0.26 pM) and rat NEP (Kd=7.0-26.8 pM). RB104 effectively blocks apNEP-mediated cleavage of Leu-enkephalin and shows minimal cross-reactivity with other zinc peptidases. Furthermore, RB104 can be iodinated or radiolabeled with 125I to serve as a probe, and is widely used in inhibitor gel electrophoresis, binding assays, Western blotting, and autoradiographic tissue localization, enabling sensitive detection of nanogram-level NEP in crude extracts and tissue sections[1][2][3][4].
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RB104 | RB104 is a highly selective neutral endopeptidase (NEP) inhibitor that exhibits extremely high affinity for Aplysia californica apNEP (Kd=0.16-0.26 pM) and rat NEP (Kd=7.0-26.8 pM). RB104 effectively blocks apNEP-mediated cleavage of Leu-enkephalin and shows minimal cross-reactivity with other zinc peptidases. Furthermore, RB104 can be iodinated or radiolabeled with 125I to serve as a probe, and is widely used in inhibitor gel electrophoresis, binding assays, Western blotting, and autoradiographic tissue localization, enabling sensitive detection of nanogram-level NEP in crude extracts and tissue sections. | |||||||||||||||||||||
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References
- [1]. Tharaux PL, et al. EGF and TGF-beta regulate neutral endopeptidase expression in renal vascular smooth muscle cells. The American journal of physiology. 1997 Jun;272(6 Pt 1):C1836-43.
- [2]. Zappulla JP, et al. Cloning and characterization of Aplysia neutral endopeptidase, a metallo-endopeptidase involved in the extracellular metabolism of neuropeptides in Aplysia californica. The Journal of neuroscience : the official journal of the Society for Neuroscience. 1999 Jun 01;19(11):4280-92. [Content Brief]
- [3]. Fournié-Zaluski MC, et al. Development of [125I]RB104, a potent inhibitor of neutral endopeptidase 24.11, and its use in detecting nanogram quantities of the enzyme by "inhibitor gel electrophoresis". Proceedings of the National Academy of Sciences of the United States of America. 1992 Jul 15;89(14):6388-92.
- [4]. Landry C, et al. Characterization of neutral endopeptidase 24.11 in dog glomeruli. The Biochemical journal. 1993 May 01;291 ( Pt 3)(Pt 3):773-9.
