Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
HDAC6
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ln Vivo |
In BAG3cKO mice, TYA-018 (15 mg/kg, oral gavage, daily, for 8 weeks) decreases Nppb expression and avoids sarcomere degradation [1].
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Animal Protocol |
Animal/Disease Models: BAG3cKO mice[1]
Doses: 15 mg/kg Route of Administration: po (oral gavage), daily, starting at 2 months old, for 8 weeks Experimental Results: Conferred cardioprotection in mice. Dramatically diminished Nppb expression to near WT. diminished fibrosis in BAG3cKO mice, although not Dramatically. partially restored protein expression of FLNC, PINK1, VDAC2, and p62 to amounts similar to WT mice. Dramatically diminished the percentage of cardiomyocytes with damaged and diminished sarcomeres in BAG3cKO mice. Dramatically diminished mitochondrial content to amounts similar to WT mice. |
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.
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Molecular Formula |
C15H13CLF2N4O3S2
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Molecular Weight |
434.87
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CAS # |
2653254-31-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
N(C1C=CC=C(C=1)Cl)(S(=O)(=O)CC)CC1=NC=C(C2=NN=C(O2)C(F)F)S1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 100 mg/mL (229.95 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.75 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.75 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.75 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2995 mL | 11.4977 mL | 22.9954 mL | |
5 mM | 0.4599 mL | 2.2995 mL | 4.5991 mL | |
10 mM | 0.2300 mL | 1.1498 mL | 2.2995 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.