Synonym
TYA-018; TYA018; TYA 018
IUPAC/Chemical Name
N-(3-chlorophenyl)-N-((5-(5-(difluoromethyl)-1,3,4-oxadiazol-2-yl)thiazol-2-yl)methyl)ethanesulfonamide
InChi Key
DAMJZODYLBMFHQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H13ClF2N4O3S2/c1-2-27(23,24)22(10-5-3-4-9(16)6-10)8-12-19-7-11(26-12)14-20-21-15(25-14)13(17)18/h3-7,13H,2,8H2,1H3
SMILES Code
O=S(N(CC1=NC=C(C2=NN=C(C(F)F)O2)S1)C3=CC(Cl)=CC=C3)(CC)=O
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
HDAC6 inhibitor
In vitro activity:
In BAG3cKO mice, TYA-018 protected against sarcomere damage and reduced Nppb expression. Based on integrated transcriptomics and proteomics and mitochondrial function analysis, TYA-018 also enhanced energetics in these mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation.
Reference:
Yang J, Grafton F, Ranjbarvaziri S, Budan A, Farshidfar F, Cho M, Xu E, Ho J, Maddah M, Loewke KE, Medina J, Sperandio D, Patel S, Hoey T, Mandegar MA. 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. Epub 2022 Jul 6. PMID: 35857625.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
434.86
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Ranjbarvaziri S, Zeng A, Wu I, Greer-Short A, Farshidfar F, Budan A, Xu E,
Shenwai R, Kozubov M, Li C, Van Pell M, Grafton F, MacKay CE, Song X, Priest JR,
Argast G, Mandegar MA, Hoey T, Yang J. Targeting HDAC6 to treat heart failure
with preserved ejection fraction in mice. Nat Commun. 2024 Feb 26;15(1):1352.
doi: 10.1038/s41467-024-45440-7. PMID: 38409164; PMCID: PMC10897156.
2: Yang J, Grafton F, Ranjbarvaziri S, Budan A, Farshidfar F, Cho M, Xu E, Ho J,
Maddah M, Loewke KE, Medina J, Sperandio D, Patel S, Hoey T, Mandegar MA.
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. Epub 2022
Jul 6. PMID: 35857625.
