Hydroxyzine pamoate
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Hydroxyzine pamoate is a histamine receptor H1 antagonist, one of the salt forms of Hydroxyzine, soluble in dimethyl formamide and chloroform but insoluble in water and alcohol.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 10246-75-0
- Formula: C44H43ClN2O8
- Molecular Weight:763.27
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
Hydroxyzine pamoate metabolite deschlorocycline induces congenital malformations[4].
Example of configuring an oral suspension of Hydroxyzine pamoate 5 mg/mL: Hydroxyzine pamoate 850 mg, Xanthan gum 1 g, Propylene glycol 5 mL, Sorbic acid 200 mg, Sorbitol solution 20 mL, Flavor q.s., Syrup q.s. to 100 mL[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mature female pregnant rats weighing 240 g[4]
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Dosage:100, 200 mg/kg
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Administration:
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Result:Showed 100 mg/kg produced 25.7% and 42.9% deformed pups per kilogram of body weight; 200 mg/kg produced 100% deformed pups per kilogram of body weight.
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Animal Model:Dog received IV hydroxyzine dihydrochloride[2][3]
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Dosage:2 mg/kg; daily; one day
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Administration:Intravenous injection (i.v.); Oral gavage (p.o.)
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Result:Showed that there was no significant difference at the 5% level in GWS (erythema×firmness×average diameter) between the two dosing methods.
Chemical Information
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CAS No. 10246-75-0
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Appearance Solid
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Molecular Weight 763.27
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Formula C44H43ClN2O8
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Color Light yellow to yellow
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SMILES
O=C(C1=C(O)C(CC2=C3C=CC=CC3=CC(C(O)=O)=C2O)=C4C=CC=CC4=C1)O.ClC5=CC=C(C(N6CCN(CCOCCO)CC6)C7=CC=CC=C7)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 250 mg/mL (327.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Tadiboyina Sirisha, et al. Enantioselective UFLC Determination of Hydroxyzine Enantiomers and Application to a Pharmacokinetic Study in Rabbits. J Chromatogr Sci. 2016 Nov;54(10):1806-1812. [Content Brief]
[2]. Petra Bizikova, et al. Blackwell Publishing Ltd Hydroxyzine and cetirizine pharmacokinetics and pharmacodynamics after oral and intravenous administration of hydroxyzine to healthy dogs. Vet Dermatol. 1966 May 1;95(1):109-11. [Content Brief]
[3]. J L Barbet, et al. Duration of inhibition of immediate skin test reactivity by hydroxyzine hydrochloride in dogs. J Am Vet Med Assoc. 1989 Jun 1;194(11):1565-9. [Content Brief]
[4]. C T King, et al. Teratogenic effect of buclizine and hydroxyzine in the rat and chlorcyclizine in the mouse. Am J Obstet Gynecol. 1966 May 1;95(1):109-11. [Content Brief]
[5]. Loyd V, et al. Hydroxyzine Pamoate 5 mg/mL Oral Suspension. US Pharm. 2014;39(5):57-58.
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 (sealed storage, away from moisture). 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 | 1.3102 mL | 6.5508 mL | 13.1015 mL | 32.7538 mL |
| 5 mM | 0.2620 mL | 1.3102 mL | 2.6203 mL | 6.5508 mL | |
| 10 mM | 0.1310 mL | 0.6551 mL | 1.3102 mL | 3.2754 mL | |
| 15 mM | 0.0873 mL | 0.4367 mL | 0.8734 mL | 2.1836 mL | |
| 20 mM | 0.0655 mL | 0.3275 mL | 0.6551 mL | 1.6377 mL | |
| 25 mM | 0.0524 mL | 0.2620 mL | 0.5241 mL | 1.3102 mL | |
| 30 mM | 0.0437 mL | 0.2184 mL | 0.4367 mL | 1.0918 mL | |
| 40 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL | |
| 50 mM | 0.0262 mL | 0.1310 mL | 0.2620 mL | 0.6551 mL | |
| 60 mM | 0.0218 mL | 0.1092 mL | 0.2184 mL | 0.5459 mL | |
| 80 mM | 0.0164 mL | 0.0819 mL | 0.1638 mL | 0.4094 mL | |
| 100 mM | 0.0131 mL | 0.0655 mL | 0.1310 mL | 0.3275 mL |