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| Targets |
ASN90 targets O-GlcNAcase (OGA), an enzyme that removes O-GlcNAc modifications from proteins. It is a potent, selective, substrate-competitive OGA inhibitor with an IC50 of 10.2 nM. The compound does not inhibit hexosaminidase (Hex), demonstrating selectivity for OGA. By inhibiting OGA, ASN90 increases O-GlcNAcylation of proteins, which is involved in neuroprotection and has implications for neurodegenerative diseases. The compound is orally active. It can be used for research of tauopathies and α-synucleinopathies.
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| ln Vitro |
In vitro studies demonstrate that ASN90 is a potent, selective, substrate-competitive O-GlcNAcase (OGA) inhibitor with an IC50 of 10.2 nM. It is a specific OGA inhibitor that does not inhibit hexosaminidase (Hex). The compound's selectivity and potency make it a valuable tool for studying O-GlcNAc biology and its role in neurodegenerative diseases. ASN90 can be used for the research of neurodegenerative diseases such as tauopathies and α-synucleinopathies. Its oral activity further supports its utility in research applications.
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| ln Vivo |
In vivo studies of ASN90 are limited in publicly available literature. As an orally active OGA inhibitor, the compound has potential for in vivo investigations of neurodegenerative diseases. O-GlcNAcylation is involved in neuroprotection and protein aggregation pathways relevant to tauopathies and α-synucleinopathies. However, specific in vivo efficacy data and detailed animal model studies are not extensively reported. Further research is needed to establish its in vivo activity profile, pharmacokinetic properties, and therapeutic potential. The compound remains a research tool for O-GlcNAc biology.
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| Enzyme Assay |
For OGA enzyme activity assays, recombinant human OGA enzyme is incubated with fluorogenic substrates (e.g., 4-methylumbelliferyl-N-acetyl-β-D-glucosaminide) and varying concentrations of ASN90. Enzyme activity is measured by fluorescence detection of the released product. IC50 values are calculated from dose-response curves. For selectivity assays, similar protocols are used with hexosaminidase (Hex) to confirm lack of inhibition. For cellular assays, cells are treated with ASN90 and O-GlcNAc levels are measured by Western blot using O-GlcNAc-specific antibodies (e.g., RL2 or CTD110.6). Assays are performed in triplicate with appropriate vehicle controls.
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| Cell Assay |
For in vitro cellular assays, neuronal cell lines or other relevant cells are cultured in appropriate media under standard conditions (37°C, 5% CO2). ASN90 is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. O-GlcNAc levels are assessed by Western blot using O-GlcNAc-specific antibodies. Protein aggregation markers (e.g., Tau phosphorylation, α-synuclein accumulation) may be measured. Cell viability and cytotoxicity are assessed using standard assays. Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
For in vivo animal studies of ASN90, no specific published protocols are available. As an orally active OGA inhibitor, the compound can be administered via oral gavage. Dosing regimens vary by study objective. In neurodegenerative disease models (e.g., tauopathy or α-synucleinopathy models), animals may be treated with compound and pathology is assessed. O-GlcNAc levels in brain tissue can be measured by Western blot. Behavioral assessments may be performed. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ASN90 indicate it is orally active. The compound has a molecular weight of 425.44, formula C23H23N5O3, and CAS number 1884154-02-2. Purity: typically high. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO and other organic solvents. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are not extensively reported in publicly available sources. The compound's oral activity supports its use in in vivo studies.
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| Toxicity/Toxicokinetics |
According to available safety information, ASN90 is intended for research purposes only. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
ASN90 (Egalognastat) is a potent, selective, substrate-competitive O-GlcNAcase (OGA) inhibitor with an IC50 of 10.2 nM. It is orally active and does not inhibit hexosaminidase (Hex). It can be used for research of neurodegenerative diseases such as tauopathies and α-synucleinopathies. It has a molecular weight of 425.44 and formula C23H23N5O3. It is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C17H21N5O3S
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| Molecular Weight |
375.445341825485
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| Exact Mass |
375.136
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| CAS # |
1884154-02-2
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| PubChem CID |
118903008
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
505
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H](C1=CC2=C(C=C1)OCO2)N3CCN(CC3)C4=NN=C(S4)NC(=O)C
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| InChi Key |
PLUUAFJXXNCXSD-NSHDSACASA-N
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| InChi Code |
InChI=1S/C17H21N5O3S/c1-11(13-3-4-14-15(9-13)25-10-24-14)21-5-7-22(8-6-21)17-20-19-16(26-17)18-12(2)23/h3-4,9,11H,5-8,10H2,1-2H3,(H,18,19,23)/t11-/m0/s1
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| Chemical Name |
N-[5-[4-[(1S)-1-(1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl]-1,3,4-thiadiazol-2-yl]acetamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6635 mL | 13.3174 mL | 26.6347 mL | |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3269 mL | |
| 10 mM | 0.2663 mL | 1.3317 mL | 2.6635 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.
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