Cat. No.: HY-12532

Astemizole

(Synonyms: R 43512)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K⁺ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects.

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Pureté: 99.77%
CAS No.: 68844-77-9
Formule: C₂₈H₃₁FN₄O
Masse moléculaire:458.57

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Astemizole Chemical Structure

CAS No.: 68844-77-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

H₁ Receptor

Voir tous les produits spécifiques à Isoform Histamine Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1.1 μM Compound: astemizole	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]
CHO	IC₅₀	29.6 μM Compound: AST	Cytotoxicity against CHO cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against CHO cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34413963]
CHO	IC₅₀	29.6 μM Compound: AST	Cytotoxicity against CHO cells measured after 48 hrs by MTT assay Cytotoxicity against CHO cells measured after 48 hrs by MTT assay	[PMID: 36507890]
HEK293	IC₅₀	0.008 μM Compound: astemizole	Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay	[PMID: 22694270]
HEK293	IC₅₀	0.023 μM Compound: Astemizole	Displacement of [3H] dofetilide from human ERG channel expressed in HEK293 cell membranes incubated for 2 hrs by scintillation counting analysis Displacement of [3H] dofetilide from human ERG channel expressed in HEK293 cell membranes incubated for 2 hrs by scintillation counting analysis	[PMID: 26985309]
HEK293	IC₅₀	0.9 nM Compound: astemizole	Inhibition of hERG potassium channel in HEK293 cells by patch clamp assay Inhibition of hERG potassium channel in HEK293 cells by patch clamp assay	[PMID: 16722631]
HEK293	IC₅₀	14 nM Compound: Astemizole	Inhibition of [3H]-astemizole binding to human ERG expressed in HEK293 cell membranes by scintillation counting method Inhibition of [3H]-astemizole binding to human ERG expressed in HEK293 cell membranes by scintillation counting method	[PMID: 29370702]
HEK293	IC₅₀	2.6 nM Compound: astemizole	Displacement of [3H]Astemizole from human recombinant ERG expressed in HEK293 cells at after 60 mins Displacement of [3H]Astemizole from human recombinant ERG expressed in HEK293 cells at after 60 mins	[PMID: 23403082]
HEK293	IC₅₀	2.6 μM Compound: Astemizole	Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay	[PMID: 32392053]
HEK293	IC₅₀	2.7 μM Compound: astemizole	Displacement of [3H]astemizole from human ERG potassium channel expressed in HEK293 cell membrane Displacement of [3H]astemizole from human ERG potassium channel expressed in HEK293 cell membrane	[PMID: 18588282]
HEK293	IC₅₀	26.4 μM Compound: astemizole	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	5.1 μM Compound: Astemizole	Cytotoxicity against human ERG transfected HEK293 cells after 24 hrs by MTT assay Cytotoxicity against human ERG transfected HEK293 cells after 24 hrs by MTT assay	[PMID: 26985309]
HepG2	IC₅₀	0.114 μM Compound: 92125178	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	[PMID: 22586124]
HepG2	IC₅₀	12 μM Compound: 92125178	HARVARD: Cytotoxicity in HepG2 cell line HARVARD: Cytotoxicity in HepG2 cell line	[PMID: 22586124]
HepG2	IC₅₀	7.97 μM Compound: Astemizole	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 30448235]
HT-29	IC₅₀	15.4 μM Compound: Astemizole	Cytotoxicity against human HT-29 cells after 24 hrs by MTT assay Cytotoxicity against human HT-29 cells after 24 hrs by MTT assay	[PMID: 26985309]
Huh-7	CC₅₀	20.89 μM Compound: GNF-Pf-2461	NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)	[PMID: 18579783]
LLC-PK1	IC₅₀	1.3 μM Compound: Astemizole	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	1.3 μM Compound: Astemizole	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	1.3 μM Compound: Astemizole	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	1.3 μM Compound: Astemizole	TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	1.7 μM Compound: Astemizole	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	1.7 μM Compound: Astemizole	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells	[PMID: 12699389]
RBL-2H3	IC₅₀	0.0533 μM Compound: Astemizole	Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method	[PMID: 31703894]
RBL-2H3	IC₅₀	0.0819 μM Compound: Astemizole	Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr	[PMID: 31703894]
RBL-2H3	IC₅₀	0.156 μM Compound: Astemizole	Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety	[PMID: 31703894]
Vero C1008	EC₅₀	1.1 μM Compound: Astemizole	Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs	[PMID: 32511357]
Vero C1008	EC₅₀	1.1 μM Compound: Astemizole	Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs	10.1101/2020.04.16.044016

In Vivo

Astemizole (p.o., 10 and 30 mg/kg) and (i.v., 1 and 3 mg/kg) has no effect on respiratory rate, heart rate and blood pressure, and even at high doses of 30 mg/kg and 3 mg/kg, also has no effect on body temperature and exercise capacity in male common marmosets. But Astemizole can prolong the QT interval and induce premature ventricular contractions at 30 mg/kg (po) and 1 mg/kg (iv)^[3].
Astemizole (p.o., 3 and 30 mg/kg) shows that the pre-drug control values (C) of the idioventricular rate, QT interval and QTcF are 31 beats/min, 319 ms and 256 at dose of 3 mg/kg, while those are 31 beats/min, 331 ms and 270 at dose of 30 mg/kg, respectively in mice. Moreover, Astemizole at a dose of 30 mg/kg (po) may cause tip-twisting ventricular tachycardia by inhibiting hERG K⁺ channels^[4].

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

Chemical Information

CAS No. 68844-77-9
Appearance Solid
Masse moléculaire 458.57
Formule C₂₈H₃₁FN₄O
Color White to off-white
SMILES

COC1=CC=C(CCN2CCC(NC3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C=C1
Synonyms

R 43512
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (9)

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ACS Nano

Single-Molecule-Based, Label-Free Monitoring of Molecular Glue Efficacies for Promoting Protein-Protein Interactions Using YaxAB Nanopores. [Abstract]

2024 Nov 12;18(45):31451-31465. PMID: 39482865
J Med Chem

Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]

2021 Mar 11;64(5):2725-2738. PMID: 33619967
Int Immunopharmacol

Histamine deficiency deteriorates LPS-induced periodontal diseases in a murine model via NLRP3/Caspase-1 pathway. [Abstract]

2023 Feb:115:109630. PMID: 36571917

Astemizole purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Feb:115:109630. [Abstract]

Astemizole (AST; 2 mg/kg; daily; intraperitoneal twice at 48 h and 24 h before LPS injection) showed that the expression levels of IL-1β and IL-6 were increased significantly in the LPS + AST group compared to the LPS group in Balb/C mice.

Astemizole purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Feb:115:109630. [Abstract]

Astemizole (AST; 2 mg/kg; daily; intraperitoneal twice at 48 h and 24 h before LPS injection) showed that the protein levels of NLRP3, Caspase-1, and Cleaved-Caspase-1 were significantly upregulated in the LPS + AST group compared to the LPS group in Balb/C mice.

Astemizole purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Feb:115:109630. [Abstract]

Astemizole (AST; 1 μM; 24 h) increased IL-1α mRNA expression in HL-60 cells treated with sodium butyrate (SB; 2 mM) and increased IL-6 mRNA expression in HGF cells treated with SB. IL-1α gene expression in HL-60 cells and (B) IL-6 gene expression in HGFs were measured by qRT-PCR.
J Mol Med (Berl)

Blocking H1R signal aggravates atherosclerosis by promoting inflammation and foam cell formation. [Abstract]

2024 Jul;102(7):887-897. PMID: 38733386
Curr Issues Mol Biol

The Antihistamine Astemizole Potentiates the Antitumor Efficacy of Sorafenib in Hepatocellular Carcinoma by Suppressing Proliferation, Metastasis, and Angiogenesis. [Abstract]

2026 May;48(5):451. PMID: 42193056
Pharm Res

Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]

2025 Aug;42(8):1315-1329. PMID: 40760405
Biochem Biophys Res Commun

Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]

2025 Oct 30:786:152756. PMID: 41043280
Biochem Biophys Res Commun

Abnormal histidine metabolism promotes macrophage lipid accumulation under Ox-LDL condition. [Abstract]

2022 Jan 15:588:161-167. PMID: 34954523

Astemizole purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2022 Jan 15:588:161-167. [Abstract]

Astemizole (AST; 1 μM; 48 h) further increased intracellular lipids (red-labeled) in the BMDMs increased after ox-LDL treatment (40 mg/mL, 48h) by Oil red O staining.

Astemizole purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2022 Jan 15:588:161-167. [Abstract]

Astemizole (AST; 1 μM; 48 h) showed that the content of the intracellular lipids (green-labeled) increased under ox-LDL condition, which was further augmented by astemizole exposure.

Astemizole purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2022 Jan 15:588:161-167. [Abstract]

Astemizole (AST; 1 μM) showed that ox-LDL significantly promoted the expression of SR-A in macrophages, which was further increased by astemizole.
SSRN

2023 Jun 27.

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (272.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1807 mL

10.9035 mL

21.8069 mL

5 mM

0.4361 mL

2.1807 mL

4.3614 mL

10 mM

0.2181 mL

1.0903 mL

2.1807 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 6.25 mg/mL (13.63 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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% Corn Oil

Solubility: ≥ 6.25 mg/mL (13.63 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

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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

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21(2):294-300. [Content Brief]

[2]. Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61. [Content Brief]

[3]. Ikuo Horii, et al. Development of telemetry system in the common marmoset--cardiovascular effects of astemizole and nicardipine. J Toxicol Sci. 2002 May;27(2):123-30. [Content Brief]

[4]. Hiroko Izumi-Nakaseko, et al. Possibility as an anti-cancer drug of astemizole: Evaluation of arrhythmogenicity by the chronic atrioventricular block canine model. J Pharmacol Sci. 2016 Jun;131(2):150-3. [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, 6 months; -20°C, 1 month. 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
DMSO	1 mM	2.1807 mL	10.9035 mL	21.8069 mL	54.5173 mL
	5 mM	0.4361 mL	2.1807 mL	4.3614 mL	10.9035 mL
	10 mM	0.2181 mL	1.0903 mL	2.1807 mL	5.4517 mL
	15 mM	0.1454 mL	0.7269 mL	1.4538 mL	3.6345 mL
	20 mM	0.1090 mL	0.5452 mL	1.0903 mL	2.7259 mL
	25 mM	0.0872 mL	0.4361 mL	0.8723 mL	2.1807 mL
	30 mM	0.0727 mL	0.3634 mL	0.7269 mL	1.8172 mL
	40 mM	0.0545 mL	0.2726 mL	0.5452 mL	1.3629 mL
	50 mM	0.0436 mL	0.2181 mL	0.4361 mL	1.0903 mL
	60 mM	0.0363 mL	0.1817 mL	0.3634 mL	0.9086 mL
	80 mM	0.0273 mL	0.1363 mL	0.2726 mL	0.6815 mL
	100 mM	0.0218 mL	0.1090 mL	0.2181 mL	0.5452 mL

Keywords

Astemizole

9 Cited Publications

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Astemizole

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Publications Citing Use of MedChemExpress (MCE) Astemizole

Voir tous les produits spécifiques à Isoform Histamine Receptor

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Astemizole Related Classifications

HY-12532 Related Classifications