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Hydroxyzine 2HCl Histamine Receptor antagonist

Name: Hydroxyzine 2HCl
Brand: Selleck Chemicals
SKU: S4026
Rating: 5 (3 reviews)

Cat.No.S4026

Hydroxyzine is a Histamine H1-receptor antagonist, inhibits binding of [³H]pyrilamine/[³H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM.

Chemical Structure

Molecular Weight: 447.83

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Quality Control

Batch: S402601 DMSO]90 mg/mL]false]Water]90 mg/mL]false]Ethanol]15 mg/mL]false Purity: 99.97%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.97

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Ebastine Ciproxifan Maleate Mianserin HCl Astemizole Lafutidine Mizolastine Rupatadine Fumarate Betahistine 2HCl

Chemical Information, Storage & Stability

Molecular Weight	447.83	Formula	C₂₁H₂₇ClN₂O₂.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2192-20-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN(CCN1CCOCCO)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl.Cl

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (200.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 90 mg/mL

Ethanol : 15 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (66.99mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Histamine H1 receptor 10 nM-19 nM
In vitro	Hydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% at 1 μM and by 17% at 0.1 μM in pretreated bladder slices for 60 min. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE). Hydroxyzine (500 µM) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 µg/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen.
In vivo	Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12167464/ [2] https://pubmed.ncbi.nlm.nih.gov/9839659/ [3] https://pubmed.ncbi.nlm.nih.gov/10884588/ [4] https://pubmed.ncbi.nlm.nih.gov/11290874/ [5] https://pubmed.ncbi.nlm.nih.gov/523173/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04188106	Completed	Smoking Cessation\|Stress\|Sleep Disturbance\|Nausea	Rose Research Center LLC\|Foundation for a Smoke Free World INC	June 17 2019	Phase 4

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