Cyclizine
Based on 1 Customer Validation
Cyclizine, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness.
For research use only. We do not sell to patients.
- Purity: 98.20%
- CAS No.: 82-92-8
- Formula: C18H22N2
- Molecular Weight:266.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>100 μM
Compound: 6
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Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis
Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis
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[PMID: 26599718] |
Cyclizine (100 μM) significantly inhibits nitrite accumulation and iNOS protein levels in the LPS-stimulated in RAW 264.7 cells supernatants[1].
Cyclizine inhibits anti-IgE-induced histamine release from isolated human lung fragments, with an IC50 of 5.42 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Naive male CDI mice (Charles River) weighing 25-30 g[3]
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Dosage:1, 10 mg/kg
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Administration:s.c.; locomotor activity (crossings) measured every 15 min for 2 hr.
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Result:Enhanced locomotor activity in a dose-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 82-92-8
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Appearance Solid
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Molecular Weight 266.38
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Formula C18H22N2
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Color White to off-white
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SMILES
CN1CCN(C(C2=CC=CC=C2)C3=CC=CC=C3)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (375.40 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. 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. 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: ≥ 2.5 mg/mL (9.39 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.39 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.
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.
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 (275 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Králová J, et, al. The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicity. Int Immunopharmacol. 2009 Jul;9(7-8):990-5. [Content Brief]
[2]. Church MK, et, al. Inhibition of histamine release from human lung in vitro by antihistamines and related drugs. Br J Pharmacol. 1980 Aug;69(4):663-7. [Content Brief]
[3]. Leza JC, et, al. Effects of antihistaminics on locomotor activity in mice. Comparison with opiate and amphetamine-induced hyperactivity. Gen Pharmacol. 1991;22(2):293-6. [Content Brief]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.7540 mL | 18.7702 mL | 37.5404 mL | 93.8509 mL |
| 5 mM | 0.7508 mL | 3.7540 mL | 7.5081 mL | 18.7702 mL | |
| 10 mM | 0.3754 mL | 1.8770 mL | 3.7540 mL | 9.3851 mL | |
| 15 mM | 0.2503 mL | 1.2513 mL | 2.5027 mL | 6.2567 mL | |
| 20 mM | 0.1877 mL | 0.9385 mL | 1.8770 mL | 4.6925 mL | |
| 25 mM | 0.1502 mL | 0.7508 mL | 1.5016 mL | 3.7540 mL | |
| 30 mM | 0.1251 mL | 0.6257 mL | 1.2513 mL | 3.1284 mL | |
| 40 mM | 0.0939 mL | 0.4693 mL | 0.9385 mL | 2.3463 mL | |
| 50 mM | 0.0751 mL | 0.3754 mL | 0.7508 mL | 1.8770 mL | |
| 60 mM | 0.0626 mL | 0.3128 mL | 0.6257 mL | 1.5642 mL | |
| 80 mM | 0.0469 mL | 0.2346 mL | 0.4693 mL | 1.1731 mL | |
| 100 mM | 0.0375 mL | 0.1877 mL | 0.3754 mL | 0.9385 mL |
Cyclizine Related Classifications
HY-B1397 Related Classifications
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