2134109-20-7
Chemical Structure
Bavarostat
Synonym(s): EKZ-001
- CAS No.: 2134109-20-7
- Formula:C20H27FN2O2
- Molecular Weight:346.44
IUPAC Name: 4-(((adamantan-1-ylmethyl)(methyl)amino)methyl)-3-fluoro-N-hydroxybenzamide
InChIKey: IGZQZELTOHAHNW-UHFFFAOYSA-N
SMILES: O=C(NO)C1=CC=C(CN(C)CC2(C3)CC4CC3CC(C4)C2)C(F)=C1
Biological Activity:
Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC50 as low as 17 nM against human HDAC6. Bavarostat can be labeled with 18F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Bavarostat | 99.51% | Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC50 as low as 17 nM against human HDAC6. Bavarostat can be labeled with 18F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers. |
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References
- [1]. Strebl MG, et al. HDAC6 Brain Mapping with [18F]Bavarostat Enabled by a Ru-Mediated Deoxyfluorination. ACS Cent Sci. 2017 Sep 27;3(9):1006-1014. [Content Brief]
- [2]. Rahal D. Translation of HDAC6 PET imaging using [18F] EKZ-001–cGMP production and measurement of HDAC6 target occupancy in NHPs–A Review[J]. 2022.
- [3]. Watson PR, et al. Aromatic Ring Fluorination Patterns Modulate Inhibitory Potency of Fluorophenylhydroxamates Complexed with Histone Deacetylase 6. Biochemistry. 2022;61(18):1945-1954. [Content Brief]
