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

Lurasidone Hydrochloride  (Synonyms: SM-13496 Hydrochloride)

製品番号: HY-B0032 純度: 99.86%
COA 取扱説明書 Technical Support

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.

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Lurasidone Hydrochloride

Lurasidone Hydrochloride 構造式

CAS 番号 : 367514-88-3

容量 価格（税別） 在庫状況 数量
5 mg $46 在庫あり
10 mg $72 在庫あり
50 mg $120 在庫あり
100 mg $180 在庫あり
200 mg $288 在庫あり
500 mg $600 在庫あり
1 g   お問い合わせ  
5 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 11 publication(s) in Google Scholar

Other Forms of Lurasidone Hydrochloride:

Lurasidone Hydrochloride 関連抗体

Top Publications Citing Use of Products

5-HT Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

Dopamine Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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製品説明

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-HT1A Receptor

 

5-HT7 Receptor

 

5-HT7 Receptor

0.495 nM (IC50)

5-HT1A Receptor

6.75 nM (IC50)

D2 Receptor

1.68 nM (IC50)

体外実験

Lurasidone (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 (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 (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].

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

Lurasidone Hydrochloride 関連抗体
体内実験

Lurasidone (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 (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 (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 (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 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

529.14

分子式

C28H37ClN4O2S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
体外: 

DMSO : 6.67 mg/mL (12.61 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.67 mg/mL (1.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 0.67 mg/mL (1.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.86%

COA (251 KB) LCMS (101 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.8899 mL 9.4493 mL 18.8986 mL 47.2465 mL
DMSO 5 mM 0.3780 mL 1.8899 mL 3.7797 mL 9.4493 mL
10 mM 0.1890 mL 0.9449 mL 1.8899 mL 4.7246 mL
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Lurasidone Hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lurasidone367514-88-3SM-13496SM13496SM 134965-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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