| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Active metabolite of lurasidone
|
|---|---|
| References |
[1]. Greenberg WM, et al. Pharmacokinetics and Pharmacodynamics of Lurasidone Hydrochloride, a Second-Generation Antipsychotic: A Systematic Review of the Published Literature. Clin Pharmacokinet. 2017 May;56(5):493-503.
|
| Additional Infomation |
Lurasidone hydrochloride is a benzisothiazol derivative, belonging to the second-generation (atypical) antipsychotic drugs. It is approved in the United States, Canada, the European Union, Switzerland, and Australia for the treatment of schizophrenia, and in the United States and Canada for the treatment of bipolar disorder. In addition to primarily antagonizing dopamine D2 receptors and serotonin 5-HT2A receptors, lurasidone also possesses unique 5-HT7 receptor antagonistic activity and exhibits partial agonistic activity against 5-HT1A receptors, while also showing mild antagonistic activity against norepinephrine α2A and α2C receptors. Lurasidone does not possess antihistamine or anticholinergic activity. The dosage for treating schizophrenia is once daily, ranging from 40 to 160 mg/day; the dosage for treating bipolar disorder is once daily, ranging from 20 to 120 mg/day. Due to its pharmacokinetic properties, it is recommended to take it with food. In healthy adult subjects and patients, a 40 mg dose reached peak plasma concentrations within 1–3 hours, with a mean elimination half-life of 18 hours (primarily excreted in feces) and an apparent volume of distribution of 6173 L; its binding to serum plasma proteins was approximately 99%. Within the approved dose range, the pharmacokinetics of lurasidone in healthy adults and clinical populations were approximately dose-proportional, as confirmed by a clinical study in children and adolescents. Lurasidone is primarily metabolized by cytochrome P450 (CYP) 3A4, with minor metabolites also present; therefore, it should not be used in combination with potent CYP3A4 inducers or inhibitors. Lurasidone does not significantly inhibit or induce CYP450 liver enzymes. [1]
|
| Molecular Formula |
C28H37CLN4O3S
|
|---|---|
| Molecular Weight |
545.14
|
| Related CAS # |
Lurasidone Hydrochloride;367514-88-3;Lurasidone;367514-87-2;Lurasidone metabolite 14326;186204-33-1
|
| PubChem CID |
137628689
|
| Appearance |
White to off-white solid
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
37
|
| Complexity |
866
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C1CC[C@H]([C@@H](C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)[C@H]6[C@H]7C[C@@H]([C@H]6C5=O)[C@H](C7)O.Cl
|
| InChi Key |
WLCWVTUFTGBTDA-GXYKJTJUSA-N
|
| InChi Code |
InChI=1S/C28H36N4O3S.ClH/c33-22-14-19-13-21(22)25-24(19)27(34)32(28(25)35)16-18-6-2-1-5-17(18)15-30-9-11-31(12-10-30)26-20-7-3-4-8-23(20)36-29-26;/h3-4,7-8,17-19,21-22,24-25,33H,1-2,5-6,9-16H2;1H/t17-,18-,19-,21+,22-,24-,25+;/m0./s1
|
| Chemical Name |
(1S,2S,6R,7S,8S)-4-[[(1R,2R)-2-[[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl]cyclohexyl]methyl]-8-hydroxy-4-azatricyclo[5.2.1.02,6]decane-3,5-dione;hydrochloride
|
| Synonyms |
Lurasidone metabolite 14326 (hydrochloride); Lurasidone metabolite 14326 hydrochloride;
|
| 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: 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) |
DMSO: ~50 mg/mL (~91.7 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (2.29 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 DMSO stock solution (12.5 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 1.25 mg/mL (2.29 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 DMSO stock solution (12.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8344 mL | 9.1720 mL | 18.3439 mL | |
| 5 mM | 0.3669 mL | 1.8344 mL | 3.6688 mL | |
| 10 mM | 0.1834 mL | 0.9172 mL | 1.8344 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
