| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) nitrosylation; also acts as an apoptosis inhibitor.
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|---|---|
| ln Vitro |
Omigapil maleate is a potent inhibitor of GAPDH nitrosylation, a post-translational modification implicated in neurodegenerative processes. It abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. The compound also acts as an apoptosis inhibitor, preventing cell death in various models.
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| ln Vivo |
Omigapilmaleate (0.1 mg/kg) treatment of mice results in increased strength and surgical regeneration [2].
In vivo, omigapil maleate demonstrates neuroprotective effects. In mouse models of Alzheimer's disease, it abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction. It has been studied in models of congenital muscular dystrophy (CMD) and shows potential for the treatment of this condition. |
| Enzyme Assay |
The inhibition of GAPDH nitrosylation by omigapil maleate is assessed using in vitro biochemical assays. Recombinant GAPDH is incubated with a nitrosylating agent in the presence of the compound, and the level of nitrosylated GAPDH is measured by specific antibodies or mass spectrometry. The inhibition of apoptosis is evaluated in cell-based models of neuronal cell death.
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| Cell Assay |
Omigapil maleate cellular activity is evaluated in neuronal cell cultures or other relevant cell types. Cells are treated with the compound and exposed to apoptotic stimuli, such as Aβ1-42 or other stressors. Cell viability is assessed by MTT or LDH release assays. Markers of apoptosis, such as caspase activation and PARP cleavage, are measured by Western blot or activity assays.
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| Animal Protocol |
Animal/Disease Models: 12weeks old dyW/mag mice [2]
Doses: 0.1 mg/kg Route of Administration: Drug treatment in the first week, one time/day, intraperitoneal (ip) injection. After weaning (3 weeks of age), take it orally one time/day. The Experimental Results:diminished muscle fiber loss. omigapil Dramatically improved many functional parameters. In vivo efficacy is studied in animal models of neurodegenerative diseases, such as transgenic mouse models of Alzheimer's disease or congenital muscular dystrophy. Omigapil maleate is administered orally at various doses. Behavioral tests (e.g., memory and locomotor function) are performed, and brain tissue is analyzed for biochemical markers of disease, such as tau acetylation and GAPDH nitrosylation. |
| ADME/Pharmacokinetics |
Omigapil maleate has a molecular formula of C23H21NO5 and a molecular weight of 391.42 g/mol. It is an orally active compound. The compound is a maleate salt and is stable when stored at -20°C. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicological data for omigapil maleate are not extensively detailed in public sources. As an apoptosis inhibitor and neuroprotective agent, it is generally well-tolerated in preclinical studies. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval.
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| References |
[1]. Sarina Meinen, et al. Apoptosis inhibitors and mini-agrin have additive benefits in congenital muscular dystrophy mice. EMBO Mol Med. 2011 Aug;3(8):465-79.
[2]. Tanusree Sen, et al. Nitrosylation of GAPDH augments pathological tau acetylation upon exposure to amyloid-β. Sci Signal. 2018 Mar 20;11(522):eaao6765. |
| Additional Infomation |
Omigapil maleate is a research compound that has been investigated in clinical trials for neurodegenerative diseases. It is not approved for clinical use. The compound is a GAPDH nitrosylation inhibitor and apoptosis inhibitor. It has been studied for congenital muscular dystrophy (CMD) and Alzheimer's disease. It is also known as CGP3466B and TCH346.
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| Molecular Formula |
C23H21NO5
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|---|---|
| Molecular Weight |
391.416546583176
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| Exact Mass |
391.142
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| CAS # |
200189-97-5
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| Related CAS # |
181296-84-4;200189-97-5;
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| PubChem CID |
9821821
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| Appearance |
White to off-white solid powder
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| LogP |
3.609
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
551
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C#CCN(CC1=CC2C=CC=CC=2OC2C=CC=CC1=2)C.OC(/C=C\C(=O)O)=O
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| InChi Key |
SQAZQLMBEHYFJA-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C19H17NO.C4H4O4/c1-3-12-20(2)14-16-13-15-8-4-6-10-18(15)21-19-11-7-5-9-17(16)195-3(6)1-2-4(7)8/h1,4-11,13H,12,14H2,2H31-2H,(H,5,6)(H,7,8)/b2-1-
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| Chemical Name |
N-(dibenzo[b,f]oxepin-10-ylmethyl)-N-methylprop-2-yn-1-amine maleate
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| Synonyms |
CGP 3466B CGP-3466B CGP3466B TCH-346 TCH 346 TCH346
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~50 mg/mL (~127.74 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (6.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 (6.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5548 mL | 12.7740 mL | 25.5480 mL | |
| 5 mM | 0.5110 mL | 2.5548 mL | 5.1096 mL | |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5548 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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