1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor
  3. Lurasidone Hydrochloride

Lurasidone Hydrochloride (Synonyms: SM-13496 Hydrochloride)

Cat. No.: HY-B0032 Purity: 99.87%
Handling Instructions

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. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

For research use only. We do not sell to patients.

Lurasidone Hydrochloride Chemical Structure

Lurasidone Hydrochloride Chemical Structure

CAS No. : 367514-88-3

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10 mM * 1 mL in DMSO USD 79 In-stock
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100 mg USD 180 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Lurasidone Hydrochloride:

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Description

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. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

IC50 & Target

5-HT7 Receptor

0.495 nM (IC50)

5-HT1A Receptor

6.75 nM (IC50)

D2 Receptor

1.68 nM (IC50)

In Vitro

Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of dopamine D2 and 5-HT7 with IC50s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. Lurasidone 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 KB value of 2.8±1.1 nM[1].

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

In Vivo

Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently increases the ratio of DOPAC/dopamine in both regions, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) (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 (Hydrochloride) (SM-13496 (Hydrochloride)) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED50 values are 6.3 mg/kg. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia with ED50 values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) (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].

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

Clinical Trial
Molecular Weight

529.14

Formula

C₂₈H₃₇ClN₄O₂S

CAS No.

367514-88-3

SMILES

O=C([[email protected]]([[email protected]]1CC[[email protected]@H]2C1)[[email protected]]2C3=O)N3C[[email protected]@H]4CCCC[[email protected]]4CN(CC5)CCN5C6=NSC7=CC=CC=C76.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.67 mg/mL (12.61 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)

Ethanol : 2 mg/mL (3.78 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (1.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (1.89 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (1.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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 (Hydrochloride) (SM-13496 (Hydrochloride)) 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].

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

References
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Keywords:

LurasidoneSM-13496SM13496SM 134965-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Product Name:
Lurasidone Hydrochloride
Cat. No.:
HY-B0032
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