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MedKoo Cat#: 326687 | Name: Lurasidone HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lurasidone HCl, also known as SM-13496, is an atypical antipsychotic drug. In the USA since 2013, it is also approved for the treatment of depressive episodes associated with bipolar I disorder as well as bipolar II disorder in adults when used alone or in combination with lithium, valproate, or lamotrigine. Lurasidone may be useful for treating the cognitive and memory deficits seen in schizophrenia. Lurasidone has activity at several serotonin receptors that are involved in learning and memory.

Chemical Structure

Lurasidone HCl
Lurasidone HCl
CAS#367514-88-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 326687

Name: Lurasidone HCl

CAS#: 367514-88-3 (HCl)

Chemical Formula: C28H37ClN4O2S

Exact Mass: 0.0000

Molecular Weight: 529.14

Elemental Analysis: C, 63.56; H, 7.05; Cl, 6.70; N, 10.59; O, 6.05; S, 6.06

Price and Availability

Size Price Availability Quantity
1g USD 150.00 2 Weeks
2g USD 250.00 2 Weeks
5g USD 450.00 2 Weeks
10g USD 750.00 2 Weeks
25g USD 1,350.00 2 Weeks
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Related CAS #
367514-88-3 (HCl) 367514-87-2 (Free base)
Synonym
SM-13496; SM 13496; SM13496; Lurasidone HCl. trade name Latuda.
IUPAC/Chemical Name
(3aR,4S,7R,7aS)-2-(((1R,2R)-2-((4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)cyclohexyl)methyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione hydrochloride
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
SMILES Code
O=C1N(C[C@H]2[C@H](CN3CCN(C4=NSC5=C4C=CC=C5)CC3)CCCC2)C([C@]6([H])[C@@](C7)([H])CC[C@@]7([H])[C@]16[H])=O.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 367514-88-3 ( Lurasidone HCl); 367514-87-2 ( Lurasidone Free base).
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively.
In vitro activity:
The inhibitory effect of the atypical neuroleptic lurasidone on the main human cytochrome P450 (CYP) enzymes in pooled human liver microsomes and cDNA-expressed CYP enzymes (supersomes) was examined. Lurasidone moderately inhibited CYP1A2 (Ki = 12.6 and 15.5 µM in microsomes and supersomes), CYP2C9 (Ki = 18 and 3.5 µM in microsomes and supersomes) and CYP2C19 via a mixed mechanism (Ki = 18 and 18.4 µM in microsomes and supersomes), and CYP3A4 via a competitive mechanism (Ki = 29.4 and 9.1 µM in microsomes and supersomes). Moreover, lurasidone competitively, though weakly diminished the CYP2D6 activity (Ki = 37.5 and 85 µM in microsomes and supersomes). Reference: Pharmacol Rep. 2020 Dec;72(6):1685-1694. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7704495/
In vivo activity:
To investigate the beneficial preclinical outcomes of lurasidone, a rat model of cranial nerve involvement model was established. The results (Fig. 2A) indicated that the total PANSS (Positive and Negative Syndrome Scale) score was significantly reduced in the rats with cranial nerve involvement treated with lurasidone compared with those treated with placebo. In addition, neuron impairment was analyzed on day 30 following lurasidone or placebo treatment. The results (Fig. 2B) showed that neuron impairment was significantly reduced in the hippocampus of lurasidone-treated mice. In addition, the risks of relapse and re-treatment in a 180-day observation period were analyzed following treatment with lurasidone, compared with the placebo. P-values were 0.00063 and 0.00048 for relapse rate and re-treatment, respectively (Fig. 2C and D). Furthermore, as shown in Fig. 2E and F, the lurasidone-treated mice had significantly higher rates of remission and reduced anxiety, compared with the placebo (P=0.0075 and P=0.0086, vs. placebo, respectively). Reference: Mol Med Rep. 2018 Apr;17(4):6002-6008. https://www.spandidos-publications.com/mmr/17/4/6002
Solvent mg/mL mM
Solubility
Ethanol 2.0 3.78
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 529.14 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Danek PJ, Wójcikowski J, Daniel WA. The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions. Pharmacol Rep. 2020 Dec;72(6):1685-1694. doi: 10.1007/s43440-020-00102-5. Epub 2020 Apr 11. PMID: 32279279; PMCID: PMC7704495. 2. He B, Yu L, Li S, Xu F, Yang L, Ma S, Guo Y. Neuroprotective effect of lurasidone via antagonist activities on histamine in a rat model of cranial nerve involvement. Mol Med Rep. 2018 Apr;17(4):6002-6008. doi: 10.3892/mmr.2018.8595. Epub 2018 Feb 13. PMID: 29436643. 3. Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S, Oki H, Tanno N, Saji I, Ito A, Ohno Y, Nakamura M. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81. doi: 10.1124/jpet.110.167346. Epub 2010 Apr 19. PMID: 20404009.
In vitro protocol:
1. Danek PJ, Wójcikowski J, Daniel WA. The atypical neuroleptics iloperidone and lurasidone inhibit human cytochrome P450 enzymes in vitro. Evaluation of potential metabolic interactions. Pharmacol Rep. 2020 Dec;72(6):1685-1694. doi: 10.1007/s43440-020-00102-5. Epub 2020 Apr 11. PMID: 32279279; PMCID: PMC7704495.
In vivo protocol:
1. He B, Yu L, Li S, Xu F, Yang L, Ma S, Guo Y. Neuroprotective effect of lurasidone via antagonist activities on histamine in a rat model of cranial nerve involvement. Mol Med Rep. 2018 Apr;17(4):6002-6008. doi: 10.3892/mmr.2018.8595. Epub 2018 Feb 13. PMID: 29436643. 2. Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S, Oki H, Tanno N, Saji I, Ito A, Ohno Y, Nakamura M. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81. doi: 10.1124/jpet.110.167346. Epub 2010 Apr 19. PMID: 20404009.
1: Awad G, Ng-Mak D, Rajagopalan K, Hsu J, Pikalov A, Loebel A. Long-term health-related quality of life improvements among patients treated with lurasidone: results from the open-label extension of a switch trial in schizophrenia. BMC Psychiatry. 2016 Jun 1;16:176. doi: 10.1186/s12888-016-0879-5. PubMed PMID: 27245981; PubMed Central PMCID: PMC4888300. 2: Lurasidone. Australas Psychiatry. 2016 Jun;24(3):313. doi: 10.1177/1039856216647220. PubMed PMID: 27231317. 3: Rajagopalan K, Bacci ED, Ng-Mak D, Wyrwich K, Pikalov A, Loebel A. Effects on health-related quality of life in patients treated with lurasidone for bipolar depression: results from two placebo controlled bipolar depression trials. BMC Psychiatry. 2016 May 23;16:157. doi: 10.1186/s12888-016-0865-y. PubMed PMID: 27215976; PubMed Central PMCID: PMC4877991. 4: Jaeschke RR, Sowa-Kućma M, Pańczyszyn-Trzewik P, Misztak P, Styczeń K, Datka W. Lurasidone: The 2016 update on the pharmacology, efficacy and safety profile. Pharmacol Rep. 2016 Apr 22;68(4):748-755. doi: 10.1016/j.pharep.2016.04.002. [Epub ahead of print] Review. PubMed PMID: 27203278. 5: Krystal AD, Zammit G. The sleep effects of lurasidone: a placebo-controlled cross-over study using a 4-h phase-advance model of transient insomnia. Hum Psychopharmacol. 2016 May;31(3):206-16. doi: 10.1002/hup.2533. Epub 2016 Apr 25. PubMed PMID: 27108672. 6: Suppes T, Kroger H, Pikalov A, Loebel A. Lurasidone adjunctive with lithium or valproate for bipolar depression: A placebo-controlled trial utilizing prospective and retrospective enrolment cohorts. J Psychiatr Res. 2016 Jul;78:86-93. doi: 10.1016/j.jpsychires.2016.03.012. Epub 2016 Mar 31. PubMed PMID: 27089521. 7: Rajagopalan K, Trueman D, Crowe L, Squirrell D, Loebel A. Cost-Utility Analysis of Lurasidone Versus Aripiprazole in Adults with Schizophrenia. Pharmacoeconomics. 2016 Jul;34(7):709-21. doi: 10.1007/s40273-016-0405-0. PubMed PMID: 27067724. 8: Correll CU, Cucchiaro J, Silva R, Hsu J, Pikalov A, Loebel A. Long-term safety and effectiveness of lurasidone in schizophrenia: a 22-month, open-label extension study. CNS Spectr. 2016 Apr 6:1-10. [Epub ahead of print] PubMed PMID: 27048911. 9: Lurasidone. Aust Prescr. 2016 Feb;39(1):25-6. doi: 10.18773/austprescr.2016.001. Epub 2015 Nov 6. Review. PubMed PMID: 27041804; PubMed Central PMCID: PMC4816874. 10: Keks NA, Hope J, Castle D. Lurasidone: an antipsychotic with antidepressant effects in bipolar depression? Australas Psychiatry. 2016 Jun;24(3):289-91. doi: 10.1177/1039856216641309. Epub 2016 Apr 1. PubMed PMID: 27036122. 11: Ghori AK, Sajatovic M, Tampi RR. A Case of Emergent Restless Legs Syndrome With Lurasidone Therapy. J Clin Psychopharmacol. 2016 Jun;36(3):293-4. doi: 10.1097/JCP.0000000000000496. PubMed PMID: 27035496. 12: Kantrowitz JT, Sharif Z, Medalia A, Keefe RS, Harvey P, Bruder G, Barch DM, Choo T, Lee S, Lieberman JA. A multicenter, rater-blinded, randomized controlled study of auditory processing-focused cognitive remediation combined with open-label lurasidone in patients with schizophrenia and schizoaffective disorder. J Clin Psychiatry. 2016 Mar 15. [Epub ahead of print] PubMed PMID: 27035157. 13: Rajagopalan K, Bacci ED, Wyrwich KW, Pikalov A, Loebel A. The direct and indirect effects of lurasidone monotherapy on functional improvement among patients with bipolar depression: results from a randomized placebo-controlled trial. Int J Bipolar Disord. 2016 Dec;4(1):7. doi: 10.1186/s40345-016-0049-1. Epub 2016 Mar 16. PubMed PMID: 26928122; PubMed Central PMCID: PMC4792823. 14: Ketter TA, Sarma K, Silva R, Kroger H, Cucchiaro J, Loebel A. LURASIDONE IN THE LONG-TERM TREATMENT OF PATIENTS WITH BIPOLAR DISORDER: A 24-WEEK OPEN-LABEL EXTENSION STUDY. Depress Anxiety. 2016 May;33(5):424-34. doi: 10.1002/da.22479. Epub 2016 Feb 26. PubMed PMID: 26918425. 15: Potkin SG, Kimura T, Guarino J. A 6-week, double-blind, placebo- and haloperidol-controlled, phase II study of lurasidone in patients with acute schizophrenia. Ther Adv Psychopharmacol. 2015 Dec;5(6):322-31. doi: 10.1177/2045125315606027. Erratum in: Ther Adv Psychopharmacol. 2015 Dec;5(6):369. PubMed PMID: 26834965; PubMed Central PMCID: PMC4722503. 16: Loebel A, Xu J, Hsu J, Cucchiaro J, Pikalov A. The development of lurasidone for bipolar depression. Ann N Y Acad Sci. 2015 Nov;1358:95-104. doi: 10.1111/nyas.12965. Review. PubMed PMID: 26771990. 17: Loebel A, Citrome L. Lurasidone: a novel antipsychotic agent for the treatment of schizophrenia and bipolar depression. BJPsych Bull. 2015 Oct;39(5):237-41. doi: 10.1192/pb.bp.114.048793. PubMed PMID: 26755968; PubMed Central PMCID: PMC4706192. 18: Calabrese F, Savino E, Papp M, Molteni R, Riva MA. Chronic mild stress-induced alterations of clock gene expression in rat prefrontal cortex: modulatory effects of prolonged lurasidone treatment. Pharmacol Res. 2016 Feb;104:140-50. doi: 10.1016/j.phrs.2015.12.023. Epub 2015 Dec 29. PubMed PMID: 26742719. 19: Chapel S, Chiu YY, Hsu J, Cucchiaro J, Loebel A. Lurasidone Dose Response in Bipolar Depression: A Population Dose-response Analysis. Clin Ther. 2016 Jan 1;38(1):4-15. doi: 10.1016/j.clinthera.2015.11.013. Epub 2015 Dec 22. PubMed PMID: 26730454. 20: Calabrese J, Rajagopalan K, Ng-Mak D, Bacci ED, Wyrwich K, Pikalov A, Loebel A. Effect of lurasidone on meaningful change in health-related quality of life in patients with bipolar depression. Int Clin Psychopharmacol. 2016 May;31(3):147-54. doi: 10.1097/YIC.0000000000000116. PubMed PMID: 26717493.