Lurasidone HCl (SM-13496)

Alias: SM13496; Lurasidone HCl; SM-13496; SM 13496; trade name Latuda
Cat No.:V1266 Purity: ≥98%
Lurasidone HCl (SM-13496; SM 13496; trade name Latuda), the hydrochloride salt of Lurasidone, is an atypical antipsychotic drug that has been approved for the treatment of schizophrenia and bipolar disorder.
Lurasidone HCl (SM-13496) Chemical Structure CAS No.: 367514-88-3
Product category: Dopamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Lurasidone HCl (SM-13496):

  • Lurasidone
  • Lurasidone Metabolite 14283-d8
  • Lurasidone metabolite 14326
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Lurasidone HCl (SM-13496; SM 13496; trade name Latuda), the hydrochloride salt of Lurasidone, is an atypical antipsychotic drug that has been approved for the treatment of schizophrenia and bipolar disorder. It acts by potently inhibiting Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50s of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and 10.8 nM, respectively.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT7 Receptor ( IC50 = 0.495 nM ); 5-HT1A Receptor ( IC50 = 6.75 nM ); D2 Receptor ( IC50 = 1.68 nM )
ln Vitro

In vitro activity: Lurasidone inhibits the binding of [35S]GTPγS at the human dopamine D2L receptor in a concentration-dependent manner with a KB value of 2.8 nM. Lurasidone, at a KB value of 2.6 nM, counteracts the accumulation of cAMP induced by 5-HT in CHO/h5-HT7 cells. Lurasidone has a maximum effect of 33% and partially stimulates [35S]GTPγS binding to the human 5-HT1A receptor membrane preparation. In the rat frontal cortex and striatum, lorazidone dose-dependently raises the ratio of DOPAC/dopamine.

ln Vivo
Lurasidone's inhibitory effects on MAP-induced hyperactivity last longer than eight hours. At one, two, four, and eight hours following treatment, the corresponding ED50 values of the action are 2.3 mg/kg, 0.87 mg/kg, 1.6 mg/kg, and 5.0 mg/kg. In rats with an ED50 of 6.3 mg/kg, lurasidone (1 mg/kg–10 mg/kg) dose-dependently inhibits the conditioned avoidance response. Rats treated with lurasidone (ED50 = 5.6 mg/kg) or 3.0 mg/kg show dose-dependent inhibition of TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia, respectively. In the Vogels conflict test, rats given a MED of 10 mg/kg receive a dose-dependent and statistically significant increase in the number of shocks (0.3 mg/kg–30 mg/kg). In rats with olfactory bulbectomy models, luerasdone (3 mg/kg, 2 weeks) dramatically reduces hyperactive behavior. The duration of the loss of righting reflexes in mice induced by hexobarbital (anesthesia) is slightly prolonged by luridodone (700 mg/kg–1000 mg/kg) in a dose-dependent manner. The MK-801-induced impairment of rats' passive-avoidance response is significantly and dose-dependently reversed by luerisdone (30 mg/kg, p.o.). In rats, MK-801-induced learning impairment in the Morris water maze test is potently reversed by luerasdone (3 mg/kg p.o.). By using the radial-arm maze test, lurasidone (3 mg/kg p.o.) potently reverses the reference memory impairment caused by MK-801 and moderately, but not significantly, attenuates the working memory impairment caused by MK-801. In the rat prefrontal cortex and, to a lesser extent, the hippocampus, lorisidone (10 mg/kg) treatment raises total BDNF mRNA levels. Without affecting the protein levels of neurotrophin (precursor and mature forms) in hippocampal extracts, luerisdone (10 mg/kg) dramatically raises the levels of mature BDNF protein in the rat prefrontal cortex.
Animal Protocol
0Methamphetamine (MAP) (1 mg/kg i.p.) is injected into each individual SD rat in a clear plastic cage one hour after the drugs or vehicle are administered. One, two, four, and eight hours prior to the MAP injection, luerazone (hydrochloride) (SM-13496 (hydrochloride)) is given as part of the persistence of effect test. Following a 10-minute MAP injection, locomotor activity is monitored for 80 minutes. The ED50 value, which inhibits MAP-induced hyperactivity by 50% of the animals tested, is determined using four or five groups of six to thirteen rats.
References

[1]. J Pharmacol Exp Ther . 2010 Jul;334(1):171-81

[2]. Eur J Pharmacol . 2007 Oct 31;572(2-3):160-70.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H37CLN4O2S
Molecular Weight
529.14
Exact Mass
528.23
Elemental Analysis
C, 63.56; H, 7.05; Cl, 6.70; N, 10.59; O, 6.05; S, 6.06
CAS #
367514-88-3
Related CAS #
Lurasidone; 367514-87-2; Lurasidone metabolite 14326 hydrochloride; Lurasidone-d8 hydrochloride; Lurasidone Metabolite 14283-d8; 2070009-43-5; Lurasidone metabolite 14326; 186204-33-1; Lurasidone Metabolite 14326-d8
Appearance
Solid powder
SMILES
C1CC[C@H]([C@@H](C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)[C@H]6[C@@H]7CC[C@@H](C7)[C@H]6C5=O.Cl
InChi Key
NEKCRUIRPWNMLK-SCIYSFAVSA-N
InChi Code
InChI=1S/C28H36N4O2S.ClH/c33-27-24-18-9-10-19(15-18)25(24)28(34)32(27)17-21-6-2-1-5-20(21)16-30-11-13-31(14-12-30)26-22-7-3-4-8-23(22)35-29-26;/h3-4,7-8,18-21,24-25H,1-2,5-6,9-17H2;1H/t18-,19+,20-,21-,24+,25-;/m0./s1
Chemical Name
(1S,2R,6S,7R)-4-[[(1R,2R)-2-[[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl]cyclohexyl]methyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dione;hydrochloride
Synonyms
SM13496; Lurasidone HCl; SM-13496; SM 13496; trade name Latuda
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 (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.67 mg/mL (1.27 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 6.7 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: ≥ 0.67 mg/mL (1.27 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 6.7 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8899 mL 9.4493 mL 18.8986 mL
5 mM 0.3780 mL 1.8899 mL 3.7797 mL
10 mM 0.1890 mL 0.9449 mL 1.8899 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.

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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.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05213143 Active
Recruiting
Drug: Lurasidone Schizophrenia Sumitomo Pharma (Suzhou) Co., Ltd. December 30, 2021 Phase 4
NCT03395392 Active
Recruiting
Drug: NRX-101
Drug: Lurasidone HCl
Bipolar Depression
Suicidal Ideation and Behavior
Second Affiliated Hospital of
Guangzhou Medical University
May 12, 2022 Phase 2
Phase 3
NCT03396068 Active
Recruiting
Drug: Lurasidone HCl
Drug: NRX-101
Bipolar Depression
Suicidal Ideation
NeuroRx, Inc. December 1, 2019 Phase 3
NCT02731612 Recruiting Drug: lurasidone
Drug: Placebo
Bipolar Disorder Nazlin Walji May 8, 2017 Phase 3
NCT05351736 Recruiting Drug: Lurasidone Schizophrenia Fondazione IRCCS Ca' Granda,
Ospedale Maggiore Policlinico
January 26, 2022 Phase 4
Biological Data
  • Lurasidone HCl

    Functional activity of lurasidone for dopamine D2L, 5-HT7, and 5-HT1A receptors.J Pharmacol Exp Ther.2010 Jul;334(1):171-81.
  • Lurasidone HCl

    Effect of lurasidone and other antipsychotics on dopamine turnover in rats: comparison in the frontal cortex and striatum.J Pharmacol Exp Ther.2010 Jul;334(1):171-81.
  • Lurasidone HCl

    Effect of lurasidone on olfactory bulbectomy-induced hyperactivity.J Pharmacol Exp Ther.2010 Jul;334(1):171-81.
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