| Identification | Back Directory | [Name]
N-(3-Chlorophenyl)-N-[[5-[5-(difluoromethyl)-1,3,4-oxadiazol-2-yl]-2-thiazolyl]methyl]ethanesulfonamide | [CAS]
2653254-31-8 | [Synonyms]
TYA-018
N-(3-Chlorophenyl)-N-[[5-[5-(difluoromethyl)-1,3,4-oxadiazol-2-yl]-2-thiazolyl]methyl]ethanesulfonamide | [Molecular Formula]
C15H13ClF2N4O3S2 | [MOL File]
2653254-31-8.mol | [Molecular Weight]
434.87 |
| Chemical Properties | Back Directory | [Boiling point ]
576.0±60.0 °C(Predicted) | [density ]
1.537±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [form ]
Solid | [pka]
-1.15±0.10(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation[1]. | [in vivo]
TYA-018 (15 mg/kg, Oral gavage, daily, for 8 weeks) protects against sarcomere damage and reduced Nppb expression in BAG3cKO mice[1]. | Animal Model: | BAG3cKO mice[1] | | Dosage: | 15 mg/kg | | Administration: | Oral gavage, daily, starting at 2 months old, for 8 weeks | | Result: | Conferred cardioprotection in mice. Significantly reduced Nppb expression to near WT. Reduced fibrosis in BAG3cKO mice, albeit not significantly. partially restored protein expression of FLNC, PINK1, VDAC2, and p62 to amounts similar to WT mice. Significantly reduced the percentage of cardiomyocytes with damaged and reduced sarcomeres in BAG3cKO mice. Significantly reduced mitochondrial content to amounts similar to WT mice. |
| [IC 50]
HDAC6 | [References]
[1] Yang J, et al. Phenotypic screening with deep learning identifies HDAC6 inhibitors as cardioprotective in a BAG3 mouse model of dilated cardiomyopathy. Sci Transl Med. 2022 Jul 6;14(652):eabl5654. DOI:10.1126/scitranslmed.abl5654 |
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| Company Name: |
NewCan Biotech Limited
|
| Tel: |
+86-0571-86912261 +86-15658003402 |
| Website: |
https://www.newcanbio.com/ |
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