Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
Other Sizes |
|
Escitalopram (Lu10171; Cipralex; Seroplex; Lu-10171; Citalopram; Lexapro; Cytalopram), the S-isomer/enantiomer of citalopram, is an approved antidepressant drug acting as a selective serotonin (5-HT) reuptake inhibitor (SSRI) with a Ki of 0.89 nM.
ln Vivo |
In stressed rats, escitalopram (10 mg/kg; intraperitoneal injection; administered daily for 28 days) lessens cognitive impairment and specifically reduces the build-up of phosphorylated tau protein [3]. Escitalopram at doses of 2.5 mg and 5 mg per day, when taken daily and for a total of 4 months, significantly decreased plaque burden by 28% and 34%, respectively [4].
|
---|---|
Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat [3]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 28 days. Experimental Results: It can selectively reduce the accumulation of phosphorylated tau protein in the hippocampus of stressed rats. And it can Dramatically relieve depression and resist the overactivity of the HPA axis in rats. Animal/Disease Models: APP-PS1 hemizygous female mice (4 months old) [4] Doses: 2.5-5 mg/kg Route of Administration: daily; drinking water for a total of 4 months Experimental Results: compared with littermates who only drank water Compared to mice, mice at both doses had Dramatically diminished plaque burden in their brains. ESC 2.5 mg/day and 5 mg/day Dramatically diminished hippocampal plaque burden by 28.7% and 34.4%, respectively. |
References |
[1]. Zhang, P., et al., Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbon itrile) analogues at monoamine transporters. J Med Chem, 2010. 53(16): p. 6112-21.
[2]. Pastoor, D. and J. Gobburu, Clinical pharmacology review of escitalopram for the treatment of depression. Expert Opin Drug Metab Toxicol, 2014. 10(1): p. 121-8. [3]. Wu C , et al. Escitalopram alleviates stress-induced Alzheimer's disease-like tau pathologies and cognitive deficits by reducing hypothalamic-pituitary-adrenal axis reactivity and insulin/GSK-3β signal pathway activity. Neurobiol Aging. 2018;67:137-147. [4]. Cirrito JR, et al. Effect of escitalopram on Aβ levels and plaque load in an Alzheimer mouse model. Neurology. 2020;95(19):e2666-e2674. |
Molecular Formula |
C19H18FN2O
|
---|---|
Molecular Weight |
309.36
|
Exact Mass |
309.1403
|
CAS # |
128196-01-0
|
Related CAS # |
Escitalopram oxalate;219861-08-2
|
SMILES |
FC1=CC=C([C@@]2(CCCN(C)C)C(C=CC(C#N)=C3)=C3CO2)C=C1
|
Synonyms |
Seroplex Escitalopram
|
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)
|
Solubility (In Vitro) |
DMSO : ~100 mg/mL (~308.27 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.71 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 (7.71 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 (7.71 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 | 3.2325 mL | 16.1624 mL | 32.3248 mL | |
5 mM | 0.6465 mL | 3.2325 mL | 6.4650 mL | |
10 mM | 0.3232 mL | 1.6162 mL | 3.2325 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.