| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
MAO-B 37.1 nM (IC50) AChE 31.8 nM (IC50)
|
|---|---|
| ln Vitro |
Neuroprotective effects of levofil (1–10 µM) hemitartrate include halting the decline of the mitochondrial membrane potential (ψ), reducing the intensity of apoptotic cascades, and reducing the generation of ROS brought on by OS insults[2]. In human neuroblastoma SK-N-SH cells, lentistigil (1–10 µM) hemitartrate has strong neuroprotective effects, such as reducing Bad and Bax gene and protein expression, inducing Bcl-2, and inhibiting caspase-3 activation[2].
|
| ln Vivo |
In the forced swim tests (FST) and elevated plus maze (EPM) tests, ladostigil (17 mg/kg; po daily for 6 weeks) hemitartrate eliminates the rats' depressive-like behavior and hyperanxiety in adulthood, from puberty to prenatally stressed rats[4]. Rats' episodic memory loss is restored in the object recognition test by ladostigil (50 μmol/kg; single po) hemitartrate[3].
|
| Animal Protocol |
Animal/Disease Models: Pathogen-free (SPF) SD (Sprague-Dawley) rats[4]
Doses: 17 mg/ kg Route of Administration: Po (added to the drinking water) daily for 6 weeks Experimental Results: Inhibited brain MAO-A and B by more than 60%. decreased hyperanxiety of male and female prenatally stressed (PS) rats in the EPM and depressive-like behavior in the FST. |
| References |
[1]. Denya I, et, al. Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease. Medchemcomm. 2018 Jan 16;9(2):357-370.
[2]. Weinreb O, et, al. Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimer's disease treatment. Curr Drug Targets. 2012 Apr;13(4):483-94. [3]. Weinstock M, et, al. Ladostigil, a novel multifunctional drug for the treatment of dementia co-morbid with depression. J Neural Transm Suppl. 2006;(70):443-6. [4]. Poltyrev T, et, al. Effect of chronic treatment with ladostigil (TV-3326) on anxiogenic and depressive-like behaviour and on activity of the hypothalamic-pituitary-adrenal axis in male and female prenatally stressed rats. Psychopharmacology (Berl). 2005 Aug;181(1):118-25. |
| Molecular Formula |
C16H20N2O2.1/2C4H6O6
|
|---|---|
| Molecular Weight |
694.77
|
| CAS # |
209394-46-7
|
| Related CAS # |
Ladostigil hydrochloride;209394-18-3;Ladostigil;209394-27-4
|
| SMILES |
C#CCN[C@@H]1CCC2=C1C=C(C=C2)OC(=O)N(C)CC.C#CCN[C@@H]1CCC2=C1C=C(C=C2)OC(=O)N(C)CC.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
|
| 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)
|
| Solubility (In Vitro) |
H2O: 100 mg/mL (143.93 mM)
DMSO: 50 mg/mL (71.97 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.80 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 12.5 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: ≥ 1.25 mg/mL (1.80 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 12.5 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: ≥ 1.25 mg/mL (1.80 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 | 1.4393 mL | 7.1966 mL | 14.3933 mL | |
| 5 mM | 0.2879 mL | 1.4393 mL | 2.8787 mL | |
| 10 mM | 0.1439 mL | 0.7197 mL | 1.4393 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
