| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
MAO-B[1]
MAO-B (monoamine oxidase B). |
|---|---|
| ln Vitro |
Tisolagiline is a potent MAO-B inhibitor with an IC50 of 7.6 nM or 8 nM. It displays 12,500-fold selectivity for MAO-B over MAO-A. This exceptional potency and selectivity make it a highly attractive candidate for therapeutic development, as it minimizes off-target effects on MAO-A.
|
| ln Vivo |
The compound is orally active and has shown efficacy in preclinical models. It is being developed for the treatment of Parkinson's disease, Alzheimer's disease, and obesity, indicating broad therapeutic potential. Its reversibility is a key feature that may offer advantages over irreversible MAO-B inhibitors in terms of safety and long-term efficacy.
|
| Enzyme Assay |
In vitro enzyme assays are performed to evaluate the inhibitory activity of Tisolagiline against MAO-B. The enzyme is incubated with a substrate and varying concentrations of the compound. The inhibition of enzyme activity is measured, and the IC50 is calculated. Its selectivity over MAO-A is assessed by comparing its activity against both isoforms.
|
| Cell Assay |
Cells expressing MAO-B are treated with Tisolagiline to assess its cellular effects. The compound's ability to inhibit MAO-B activity in intact cells is measured. Its effects on neurotransmitter levels and cellular signaling are evaluated to understand its mechanism of action.
|
| Animal Protocol |
In vivo studies are conducted in animal models of Parkinson's disease, Alzheimer's disease, and obesity to evaluate the therapeutic potential of Tisolagiline. The compound is administered orally due to its oral activity. Its effects on motor function, cognitive performance, and metabolic parameters are assessed.
|
| ADME/Pharmacokinetics |
Tisolagiline is an orally active compound. As a drug candidate, its pharmacokinetic properties would have been extensively characterized in preclinical studies. These would include parameters such as oral bioavailability, half-life, volume of distribution, and brain penetration to support its development for CNS indications.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available. However, its development for human therapeutic use implies that it has undergone preclinical safety assessments. Its high selectivity for MAO-B suggests a potentially favorable safety profile, with a reduced risk of the "cheese effect" associated with MAO-A inhibition.
|
| References | |
| Additional Infomation |
Tisolagiline is a small molecule drug. The INN stem "-giganin" in its name indicates that tisolagiline is a monoamine oxidase type B (MAO) inhibitor. The monoisotope molecular weight of tisolagiline is 322.13 Da.
Tisolagiline (KDS2010) is a clinical-stage MAO-B inhibitor being developed for various CNS and metabolic disorders. Its exceptional potency (IC50 = 7.6 nM) and selectivity (>12,500-fold over MAO-A) distinguish it from other MAO-B inhibitors. It has the potential to address the limitations of existing therapies, particularly in maintaining long-term efficacy. It is not yet approved for clinical use. |
| Molecular Formula |
C18H21F3N2O4S
|
|---|---|
| Molecular Weight |
418.430554151535
|
| Exact Mass |
322.129
|
| CAS # |
1894207-44-3
|
| PubChem CID |
132023446
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.1
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
384
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
S(C)(=O)(=O)O.FC(C1C=CC(=CC=1)C1C=CC(=CC=1)CN[C@H](C(N)=O)C)(F)F
|
| InChi Key |
XCUXYNYVUMLDKH-NSHDSACASA-N
|
| InChi Code |
InChI=1S/C17H17F3N2O/c1-11(16(21)23)22-10-12-2-4-13(5-3-12)14-6-8-15(9-7-14)17(18,19)20/h2-9,11,22H,10H2,1H3,(H2,21,23)/t11-/m0/s1
|
| Chemical Name |
(2S)-2-[[4-[4-(trifluoromethyl)phenyl]phenyl]methylamino]propanamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (310.25 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3899 mL | 11.9494 mL | 23.8989 mL | |
| 5 mM | 0.4780 mL | 2.3899 mL | 4.7798 mL | |
| 10 mM | 0.2390 mL | 1.1949 mL | 2.3899 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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