Mequitazine (Synonyms: LM-209)

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

Cat. No.: HY-B2168 Purity: 99.97%: FAQs
Data Sheet SDS COA 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	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 190	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-d₈ hydrobromide Get quote
Mequitazine (Standard) Get quote

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View All Isoforms

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 : 16 mg/mL (49.62 mM; Need ultrasonic and warming; 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.

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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 Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.99%

Select Batch:

Data Sheet (279 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

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

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View All Histamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Mequitazine Related Antibodies

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Complete Stock Solution Preparation Table

Mequitazine Related Classifications

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