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Lurasidone Metabolite 14283 hydrochloride is an inactive metabolite of Lurasidone which is an atypical antipsychotic drug approved for the treatment of schizophrenia and bipolar disorders.
| Targets |
Active metabolite of Lurasidone
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| References |
[1]. Lurasidone : in the treatment of schizophrenia. CNS Drugs. 2013 Jan;27(1):67-80.
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| Additional Infomation |
This review focuses on the efficacy and tolerability of lurasidone. Lurasidone is approved for the treatment of schizophrenia in the United States, Puerto Rico, and Canada. In two placebo-controlled Phase II clinical trials, 40–120 mg of lurasidone daily effectively reduced acute symptoms of schizophrenia. In a third Phase II clinical trial, there were no significant differences between the lurasidone group and the placebo group in key endpoints, neither the lurasidone group nor the haloperidol control group. In two placebo- and active-drug-controlled Phase III clinical trials, 40–160 mg of lurasidone daily, 15 mg of olanzapine daily, and 600 mg of quetiapine extended-release tablets daily all effectively reduced symptoms of schizophrenia. In a 12-month double-blind extension trial, the relapse rate in the lurasidone group was non-inferior to that in the quetiapine extended-release tablet group. In a third Phase III trial, 80 mg of lurasidone daily (instead of 40 mg or 120 mg daily) was superior to placebo in the primary endpoint. In an unpublished trial, there were no significant differences in the primary endpoint among the lurasidone group, the active control group, and the placebo group. Lurasidone was generally well tolerated in both the short and long term. Extrapyramidal symptoms and akathisia occurred in approximately 10–13% of patients. Lurasidone was associated with a lower risk of QT interval prolongation, weight gain, metabolic disorders, and hyperprolActeinemia. Further comparative trials with other antipsychotics are needed to fully assess its efficacy and tolerability. [1]
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| Molecular Formula |
C28H36N4O3S.HCL
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|---|---|
| Molecular Weight |
545.13638
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| Exact Mass |
544.227
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| CAS # |
186204-32-0
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| Related CAS # |
186204-31-9
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| PubChem CID |
129011992
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| Appearance |
White to off-white solid powder
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| LogP |
3.969
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
37
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| Complexity |
866
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| Defined Atom Stereocenter Count |
7
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| SMILES |
O=C([C@]([C@@H]1C[C@@H](O)[C@H]2C1)([H])[C@]2([H])C3=O)N3C[C@H]4[C@H](CN(CC5)CCN5C6=NSC7=C6C=CC=C7)CCCC4.Cl[H]
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| InChi Key |
WLCWVTUFTGBTDA-HRKUQYLCSA-N
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| 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
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| Chemical Name |
(1S,2S,6R,7S,8R)-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
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| Synonyms |
186204-32-0; Lurasidone Metabolite 14283 hydrochloride; Lurasidone Inactive Metabolite 14283; (1S,2S,6R,7S,8R)-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; LurasidoneMetabolite14283HCl;
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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) |
Ethanol : ~100 mg/mL (~183.44 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.59 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (4.59 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (4.59 mM) (saturation unknown) in 10% EtOH + 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 | 1.8344 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.
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