| Field | Specification |
|---|---|
| Alternative names | ORY-2001 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H20N4O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Vafidemstat, also known as ORY-2001, is an oral, brain-penetrant, dual inhibitor of lysine-specific histone demethylase 1 (LSD1) and MAO-B[1]. It is supplied as a white to off-white solid (C19H20N4O2, MW 336.39) at 98.03% purity.
Physical & Chemical Properties
| CAS Number | 1357362-02-7 |
|---|---|
| Molecular Formula | C19H20N4O2 |
| Molecular Weight | 336.39 g/mol |
| Purity | 98.03% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | NC1=NN=C(O1)CN[C@H]2[C@H](C3=CC=C(OCC4=CC=CC=C4)C=C3)C2 |
| Signaling Pathway | Epigenetics; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 50 mg/mL (148.64 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. ORYZON presents data on the Phase I trial with ORY-2001 at the 13th International Conference on Alzheimer’s and Parkinson’s diseases
[2]. ORYZON Reports Financial Results and Corporate Update for the 1st Half Ended June 30, 2018.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (148.64 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 5 mg/mL (14.86 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 5 mg/mL (14.86 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (14.86 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Vafidemstat (ORY-2001) is a dual LSD1/MAO-B inhibitor and a novel epigenetic agent for treating neurodegenerative diseases. LSD1 is a protein that takes part in transcription regulation complexes; modulating it can be used to adjust transcriptional imbalances in neurodegenerative disease and to address neuroinflammation and cognitive deficit[1]. Vafidemstat (ORY-2001) can be used to treat Alzheimer's disease[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. Clin Exp Med 2025 Nov 25;26(1):33. PMID: 41286164
Heterozygous Kmt2d loss diminishes enhancers to render medulloblastoma cells vulnerable to combinatory inhibition of lysine demethylation and oxidative phosphorylation. bioRxiv 2023 Nov 9:2023.10.29.564587. PMID: 37961118
