製品番号: HY-14543

Sertindole

(別名: Lu 23-174)

3 Cited Publications

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Sertindole (Lu 23-174) is an orally active 5-HT_2A, 5-HT_2C, dopamine D₂, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.92%
CAS 番号: 106516-24-9
分子式: C₂₄H₂₆ClFN₄O
分子量:440.94

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Sertindole 構造式

CAS 番号: 106516-24-9

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (3)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

5-HT_2A Receptor

5-HT_2C Receptor

5-HT Receptor アイソフォーム固有の製品をすべて表示 :

Dopamine Receptor アイソフォーム固有の製品をすべて表示 :

Adrenergic Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	2.7 nM Compound: sertindole	Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay	[PMID: 24805037]
CHO	IC₅₀	3 nM Compound: Sertindole	Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1	[PMID: 12729675]
CHO	IC₅₀	6.3 μM Compound: sertindole	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]

体外実験

Sertindole (0-100 μM; 48 h) attenuates proliferation of breast cancer cells^[2].
Sertindole (0.8-27.6 μM; 48 h) inhibits proliferation toward many cancers in vitro^[2].
Sertindole (5 μΜ and 10 μΜ; 24 h) attenuates migration of breast cancer cells^[2].

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

Cell Proliferation Assay^[2]

Cell Line:

SUM159 and MCF-10A cells
Concentration:

0-100 μM
Incubation Time:

48 hours
Result:

Showed IC₅₀s of 9.2 µM and 27.6 µM for SUM159 and MCF-10A cells, respectively.

Cell Proliferation Assay^[2]

Cell Line:

NCI-H460, A549, NCI-H446, NCI-H661, 801-D, U251, A172, U118-MG, U87-MG, AGS, MKN45, BGC-823, SGC-7901, HT-29, COLO205, SW480, SW620, HCT-15, HepG2, Bel-7402, MCF-7, MDA-MB-231, SUM159, T47D, MDA-MB-453, ZR-75-1, CCRF-CEM, K562, Jurkat, MCF-10A cells
Concentration:

0.8-27.6 μM
Incubation Time:

48 hours
Result:

Showed IC₅₀s ranging between 0.8-12.7 µM, 2.7-4.6 µM, 12.7-15.3 µM and 8.6-16.1 µM for breast cancer, leukemia, hepatoma and glioblastoma lines, respectively.

Cell Migration Assay ^[2]

Cell Line:

SUM159 cells
Concentration:

5 μΜ and 10 μΜ
Incubation Time:

24 hours
Result:

Blocked around 50% cells traversing the membranes at 5 μΜ, and almost all the cells lost traversing ability at 10 μΜ.
Elevated LC3II conversion significantly (P < 0.01).

体内実験

Sertindole (oral gavage; 10 mg/kg; once daily; 12 d) shows anti-tumor activity in vivo^[2].

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

Animal Model:

Immune-deficient Balb/c mice implanted MDA-MB-231 human TNBC cells^[2]
Dosage:

10 mg/kg
Administration:

Oral gavage; 10 mg/kg; once daily; 12 days
Result:

Exhibited a 22.7% reduction in size after a 12-day administration regimen.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 106516-24-9
性状 Solid
分子量 440.94
分子式 C₂₄H₂₆ClFN₄O
Color White to off-white
SMILES

FC1=CC=C(N2C3=CC=C(Cl)C=C3C(C4CCN(CCN5CCNC5=O)CC4)=C2)C=C1
別名

Lu 23-174
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Microsyst Nanoeng

A biosensing system using a multiparameter nonlinear dynamic analysis of cardiomyocyte beating for drug-induced arrhythmia recognition. [Abstract]

2022 May 9;8:49. PMID: 35547605
Eur J Pharm Sci

Repurposing of FDA-approved drugs by targeting SIRT2 to alleviate inflammatory response and kidney injury. [Abstract]

2025 Sep 27:214:107296. PMID: 41022315
ACS Omega

Antibacterial and Antibiofilm Activities of Sertindole and Its Antibacterial Mechanism against Staphylococcus aureus. [Abstract]

2023 Feb 3;8(6):5415-5425. PMID: 36816695

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (56.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.2679 mL

11.3394 mL

22.6788 mL

5 mM

0.4536 mL

2.2679 mL

4.5358 mL

10 mM

0.2268 mL

1.1339 mL

2.2679 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (282 KB)
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COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. David Murdoch, et al. Sertindole : a review of its use in schizophrenia. CNS Drugs. 2006;20(3):233-55. [Content Brief]

[2]. Wei Zhang, et al. Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. Sci Rep. 2018 Oct 25;8(1):15753. [Content Brief]

[3]. Mario F Juruena, et al. Sertindole in the management of schizophrenia. J Cent Nerv Syst Dis. 2011 May 17;3:75-85. [Content Brief]

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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2679 mL	11.3394 mL	22.6788 mL	56.6971 mL
	5 mM	0.4536 mL	2.2679 mL	4.5358 mL	11.3394 mL
	10 mM	0.2268 mL	1.1339 mL	2.2679 mL	5.6697 mL
	15 mM	0.1512 mL	0.7560 mL	1.5119 mL	3.7798 mL
	20 mM	0.1134 mL	0.5670 mL	1.1339 mL	2.8349 mL
	25 mM	0.0907 mL	0.4536 mL	0.9072 mL	2.2679 mL
	30 mM	0.0756 mL	0.3780 mL	0.7560 mL	1.8899 mL
	40 mM	0.0567 mL	0.2835 mL	0.5670 mL	1.4174 mL
	50 mM	0.0454 mL	0.2268 mL	0.4536 mL	1.1339 mL

Sertindole

3 Cited Publications

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Sertindole

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MedChemExpress（MCE）の使用を引用している文献 Sertindole

5-HT Receptor アイソフォーム固有の製品をすべて表示

Dopamine Receptor アイソフォーム固有の製品をすべて表示

Adrenergic Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (3)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Sertindole 関連分類

HY-14543 関連分類