Art. -Nr.: HY-B0032A

Lurasidone

(Synonyms: SM-13496)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

Lurasidone (SM-13496) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

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Reinheit: 99.92%
CAS. Nr.: 367514-87-2
Formel: C₂₈H₃₆N₄O₂S
Molecular Weight:492.68

Speicherung:

4°C, protect from light

* The compound is unstable in solutions, freshly prepared is recommended.

Lurasidone Chemical Structure

CAS. Nr.: 367514-87-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

5-HT_1A Receptor

5-HT₇ Receptor

0.495 nM (IC₅₀)

5-HT_1A Receptor

6.75 nM (IC₅₀)

D₂ Receptor

1.68 nM (IC₅₀)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Lurasidone (SM-13496) is an antagonist of dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone (SM-13496) demonstrates affinity for dopamine D₂ and 5-HT_2A receptors higher than other tested antipsychotics. Lurasidone (SM-13496) does not increase [³⁵S]GTPγS binding to the membrane preparations for dopamine D₂ receptors by itself, but it antagonizes dopamine-stimulated [³⁵S]GTPγS binding in a concentration-dependent manner with a K_B value of 2.8±1.1 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Lurasidone (SM-13496) dose-dependently increases the ratio of DOPAC/dopamine in frontal cortex and striatum, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (SM-13496) (ED₅₀ values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED₅₀ values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED₅₀ 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED₅₀ values 0.44 to 1.7 mg/kg). Lurasidone (SM-13496) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED₅₀ values are 6.3 mg/kg. Lurasidone (SM-13496) dose-dependently inhibits tryptamine (TRY)-induced forepaw clonic seizure and p-chloroamphetamine (p-CAMP)-induced hyperthermia with ED₅₀ values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (SM-13496) (0.3 to 30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the conflict test with MED of 10 mg/kg (p<0.01)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 367514-87-2
Appearance Solid
Molecular Weight 492.68
Formel C₂₈H₃₆N₄O₂S
Color White to off-white
SMILES

O=C([C@H]1[C@H]2C[C@H](CC2)[C@@H]31)N(C[C@H](CCCC4)[C@@H]4CN5CCN(CC5)C6=NSC7=CC=CC=C67)C3=O
Synonyms

SM-13496
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (11)

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Journal Impact Factor

Nature

Ligand recognition and G protein coupling of trace amine receptor TAAR1. [Abstract]

2023 Dec;624(7992):672-681. PMID: 37935376
Nat Immunol

Microbiota-shaped neutrophil senescence regulates sexual dimorphism in bladder cancer. [Abstract]

2025 Apr 11. PMID: 40217111
J Med Chem

Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist. [Abstract]

2024 Apr 25;67(8):6144-6188. PMID: 38593423
Antibiotics (Basel)

NRX-101 (D-Cycloserine + Lurasidone) Is Active against Drug-Resistant Urinary Pathogens In Vitro. [Abstract]

2024 Mar 28;13(4):308. PMID: 38666984
ACS Chem Neurosci

Discovery of Procognitive Antipsychotics by Combining Muscarinic M1 Receptor Structure-Activity Relationship with Systems Response Profiles in Zebrafish Larvae. [Abstract]

2020 Jan 15;11(2):173-183. PMID: 31850734
Physiol Behav

Voluntary wheel running improves cognitive deficits and abnormal agonistic behavior induced by social isolation stress in mice. [Abstract]

2026 Feb:304:115176. PMID: 41242457
J Ocul Pharmacol Ther

Survey of Dopamine Receptor D2 Antagonists as Retinal Antifibrotics. [Abstract]

2024 Oct;40(8):536-542. PMID: 39206555
bioRxiv

2025 Sep 9.
bioRxiv

2024 Jan 14.
Marmara Pharm J

2017;21 (4): 931-937.
Marmara Pharm J

2017;21 (4): 931-937.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20.83 mg/mL (42.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 3.33 mg/mL (6.76 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0297 mL

10.1486 mL

20.2972 mL

5 mM

0.4059 mL

2.0297 mL

4.0594 mL

10 mM

0.2030 mL

1.0149 mL

2.0297 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[1]

SD rats are individually isolated in clear plastic cages and injected with methamphetamine (MAP) (1 mg/kg i.p.) 1 h after the administration of drugs or vehicle. In the test of persistence of the effect, Lurasidone (SM-13496) is administered 1, 2, 4, and 8 h before the MAP injection. Locomotor activity is measured for 80 min from 10 min after MAP injection. Four or five groups of 6 to 13 rats are used to calculate the ED₅₀ value that inhibits MAP-induced hyperactivity by 50% of the animals tested^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ishibashi T, et al. 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. [Content Brief]

[2]. Sakine Atila Karaca, et al. Development of a validated high-performance liquid chromatographic method for the determination of Lurasidone in pharmaceuticals. Marmara Pharm J. 2017;21 (4): 931-937.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.0297 mL	10.1486 mL	20.2972 mL	50.7429 mL
Ethanol / DMSO	5 mM	0.4059 mL	2.0297 mL	4.0594 mL	10.1486 mL
DMSO	10 mM	0.2030 mL	1.0149 mL	2.0297 mL	5.0743 mL
	15 mM	0.1353 mL	0.6766 mL	1.3531 mL	3.3829 mL
	20 mM	0.1015 mL	0.5074 mL	1.0149 mL	2.5371 mL
	25 mM	0.0812 mL	0.4059 mL	0.8119 mL	2.0297 mL
	30 mM	0.0677 mL	0.3383 mL	0.6766 mL	1.6914 mL
	40 mM	0.0507 mL	0.2537 mL	0.5074 mL	1.2686 mL

Keywords

Lurasidone

11 Cited Publications

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Lurasidone

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Lurasidone

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lurasidone

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Lurasidone

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lurasidone Related Classifications

HY-B0032A Related Classifications