Mequitazine (Synonyms: LM-209)

Name: Mequitazine
Brand: MedChemExpress
SKU: HY-B2168
Rating: 4.5 (1 reviews)

Cat. No.: HY-B2168 Purity: 99.97%: Data Sheet
COA

SDS
Handling Instructions
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Mequitazine is a potent, and long-acting histamine H₁ antagonist.

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

Mequitazine Chemical Structure

CAS No. : 29216-28-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
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
25 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

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Mequitazine:

Mequitazine (Standard) In-stock
Mequitazine-d₈ hydrobromide Get quote

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Mequitazine is a potent, and long-acting histamine H₁ antagonist.

Cellular Effect

Cell Line	Type	Value	Description	References
Vero	CC₅₀	27.34 μM Compound: Mequitazine	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	7.28 μM Compound: Mequitazine	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Mequitazine is a potent H₁-receptors selective antihistaminic drug widely studied and used for allergic disorders such as hay fever and urticaria^[1]. Mequitazine demonstrates significant bactericidal effects against all the tested clinical isolates including Ps. aeruginosa. Its effect against the Gram-positive isolates is more pronounced^[2].

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

In Vivo

Mequitazine and clemizole antagonize the effect of histamine in guinea-pig ileum competitively. Mequitazine at 10⁷ produces a parallel shift of the dose-response curve to acetylcholine in the rat duodenum. Mequitazine at highest concentration shows anticholinergic activity^[3]. Mequitazine inhibits contractile responses to KCl, phenylephrine (PE), 5-hydroxytryptamine (5-HT), and Ca²⁺ in rat aorta^[4].

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

Molecular Weight

322.47

Formula

C₂₀H₂₂N₂S

CAS No.

29216-28-2

Appearance

Solid

Color

White to off-white

SMILES

C12=CC=CC=C1N(CC3CN4CCC3CC4)C5=C(C=CC=C5)S2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (155.05 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	3.1011 mL	15.5053 mL	31.0106 mL
5 mM	0.6202 mL	3.1011 mL	6.2021 mL
10 mM	0.3101 mL	1.5505 mL	3.1011 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, 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.

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: ≥ 2.5 mg/mL (7.75 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.
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: ≥ 2.5 mg/mL (7.75 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.
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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.75 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

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: 99.99%

Select Batch:

Data Sheet (280 KB) SDS (479 KB)

COA (257 KB) LCMS (119 KB)

Handling Instructions (2659 KB)

References

[1]. Gonnot V, et al. Expedient synthesis of mequitazine an antihistaminic drug by palladium catalyzed allylic alkylation of sodium phenothiazinate. Chem Pharm Bull (Tokyo). 2009 Nov;57(11):1300-2. [Content Brief]

[2]. El-Nakeeb MA, et a. In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates. Braz J Microbiol. 2011 Jul;42(3):980-91. [Content Brief]

[3]. Martinez-Mir I, et al. Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole. J Pharm Pharmacol. 1988 Sep;40(9):655-6. [Content Brief]

[4]. Satake N, et al. Possible mechanisms of vasoinhibitory effects of mequitazine, an antiallergic agent, on the contractions of isolated rat aorta induced by K+, phenylephrine, 5-hydroxytryptamine, and Ca2+. J Cardiovasc Pharmacol. 1994 Apr;23(4):669-73. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1011 mL	15.5053 mL	31.0106 mL	77.5266 mL
	5 mM	0.6202 mL	3.1011 mL	6.2021 mL	15.5053 mL
	10 mM	0.3101 mL	1.5505 mL	3.1011 mL	7.7527 mL
	15 mM	0.2067 mL	1.0337 mL	2.0674 mL	5.1684 mL
	20 mM	0.1551 mL	0.7753 mL	1.5505 mL	3.8763 mL
	25 mM	0.1240 mL	0.6202 mL	1.2404 mL	3.1011 mL
	30 mM	0.1034 mL	0.5168 mL	1.0337 mL	2.5842 mL
	40 mM	0.0775 mL	0.3876 mL	0.7753 mL	1.9382 mL
	50 mM	0.0620 mL	0.3101 mL	0.6202 mL	1.5505 mL
	60 mM	0.0517 mL	0.2584 mL	0.5168 mL	1.2921 mL
	80 mM	0.0388 mL	0.1938 mL	0.3876 mL	0.9691 mL
	100 mM	0.0310 mL	0.1551 mL	0.3101 mL	0.7753 mL

Mequitazine 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:

Mequitazine29216-28-2LM-209LM209LM 209Histamine ReceptorInhibitorinhibitorinhibit

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Mequitazine (Synonyms: LM-209)

Customer Review

Other Forms of Mequitazine:

Mequitazine Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Mequitazine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Mequitazine Related Classifications

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