Astemizole (Synonyms: R 43512)

Name: Astemizole
Brand: MedChemExpress
SKU: HY-12532
Rating: 5.0 (6 reviews)

Cat. No.: HY-12532 Purity: 99.77%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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.

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

Astemizole Chemical Structure

CAS No. : 68844-77-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Astemizole:

Astemizole-d3 Get quote
Astemizole (Standard) Get quote

6 Publications Citing Use of MCE Astemizole

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

H₁ 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 measured after 48 hrs by MTT assay Cytotoxicity against CHO cells measured after 48 hrs by MTT assay	[PMID: 36507890]
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]
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	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	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]
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	1.7 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]
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]

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.

Molecular Weight

458.57

Formula

C₂₈H₃₁FN₄O

CAS No.

68844-77-9

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 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.
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% 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

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (253 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Astemizole Related Classifications

Inflammation/Immunology Endocrinology

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:

Astemizole68844-77-9R 43512R43512R-43512Histamine ReceptorPotassium ChannelKcsAantihistamine drughistamine H1-receptorhERG K+antipruriticInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Requested Quantity *
Applicant Name *			Salutation
Email Address *			Phone Number *
Department			Organization Name *
City			State
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Astemizole (Synonyms: R 43512)

Customer Review

Other Forms of Astemizole:

Astemizole Related Antibodies

6 Publications Citing Use of MCE Astemizole

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Astemizole Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report