[CAS NO. 367514-87-2] lurasidone

Name: lurasidone
Brand: Arctom Scientific
SKU: SLK-S5714

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PRODUCTS SPECIFICATIONS [367514-87-2]

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Catalog

SLK-S5714

Brand

Selleck

CAS

367514-87-2

DESCRIPTION [367514-87-2]

Overview

MDL	-
Molecular Weight	492.68
Molecular Formula	C28H36N4O2S
SMILES	O=C1[C@]2([C@]([C@H]3C[C@@H]2CC3)(C(=O)N1C[C@H]4[C@H](CN5CCN(CC5)C=6C=7C(SN6)=CC=CC7)CCCC4)[H])[H]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
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
50 mM	-	-	-

Description

Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at and receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for (Ki = 0.5 nM), partial agonist activity at (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.

Targets

5-HT2A ^[1] (Cell-free assay)	5-HT7 receptor ^[1] (Cell-free assay)	D2 receptor ^[1] (Cell-free assay)	5-HT1A receptor ^[1] (Cell-free assay)
0.5 nM(Ki)	0.5 nM(Ki)	1 nM(Ki)	6.4 nM(Ki)

In vitro

Lurasidone is a new atypical antipsychotic in the benzoisothiazoles class of chemicals. Like most second-generation antipsychotics it is a full antagonist at dopamine D2 and serotonin 5-HT2A receptors, and is a partial agonist at 5-HT1A receptors. It has much greater affinity for 5-HT7 subtype receptors than other atypical antipsychotics. Lurasidone also has high affinity for the 5-HT1A subtype, α2c-adrenergic receptors and low affinity for α1-adrenergic receptors. It has minimal affinity for 5-HT2C receptors and negligible affinity for histamine H1 and muscarinic receptors.

In vivo

Lurasidone is rapidly absorbed, reaching peak concentrations within 1.5–3 hours (tmax) after single and multiple oral doses. Once absorbed, it extensively distributes in tissues and rapidly enters the CNS. Lurasidone has high binding to human plasma albumin and alpha-1-glycoprotein (≥99%). Long-term treatment of schizophrenia with lurasidone has been shown to reduce the risk of relapse. The elimination half-life of lurasidone is about 20-40 h. Mean Cmax and area under the curve (AUC) for lurasidone were approximately threefold and twofold greater, respectively, in a comparison of administration with food v. fasting. Lurasidone absorption is independent of food fat content. Lurasidone is metabolised primarily via CYP3A4. In animal studies, lurasidone penetrated the placental barrier and distributed into the fetus, and was excreted in milk during lactation.

References

[1] Antony Loebel, et al. BJPsych Bull. 2015, 39(5): 237–241.
[2] Caccia S, et al. Neuropsychiatr Dis Treat. 2012, 8:155-68.

Synonyms

4,7-Methano-1H-isoindole-1,3(2H)-dione, 2-[[(1R,2R)-2-[[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]methyl]hexahydro-, (3aR,4S,7R,7aS)-

(3aR,4S,7R,7aS)-2-[[(1R,2R)-2-[[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]methyl]hexahydro-4,7-methano-1H-isoindole-1,3(2H)-dione

Lurasidone

2-[[(1R,2R)-2-[[4-(1,2-Benzoisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]methyl]hexahydro-(3aS,4R,7S,7aR)-4,7-methano-1H-isoindole-1,3(2H)-dione