Quipazine
Based on 1 Customer Validation
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 97.0%
- CAS. Nr.: 4774-24-7
- Formel: C13H15N3
- Molecular Weight:213.28
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NG108-15 | EC50 |
1 nM
Compound: 2
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Effective concentration against 5-Hydroxytryptamine 3 receptor by measuring [14C]guanidinium uptake on NG108-15 cells.
Effective concentration against 5-Hydroxytryptamine 3 receptor by measuring [14C]guanidinium uptake on NG108-15 cells.
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[PMID: 10543880] |
| NG108-15 | EC50 |
25 nM
Compound: 4a
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Quantitative effect on the [14C]guanidinium accumulation in NG 108-15 cells.
Quantitative effect on the [14C]guanidinium accumulation in NG 108-15 cells.
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[PMID: 10229626] |
| NG108-15 | EC50 |
25 nM
Compound: quipazine
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Effective concentration for uptake of [14C]guanidinium on NG108-15 cells
Effective concentration for uptake of [14C]guanidinium on NG108-15 cells
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[PMID: 9357534] |
Quipazine shows binding efficacy to 5-HT1 and 5-HT2 with Ki values of 230 nM[3]. Quipazine displaces [3H]GR65630 from 5-HT3R in rat entorhinal cortex with a Ki value of 1.4 nM[3]. Quipazine shows antagonistic properties on the rat vagus nerve with pIC50 value of 6.1, 6.49 and 6.17 for 5-HT2, 5-HT1 and inhibition of 5-HT release[4].
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.
Chemical Information
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CAS. Nr. 4774-24-7
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Appearance Solid
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Molecular Weight 213.28
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Formel C13H15N3
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Color Off-white to light yellow
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SMILES
C1(N2CCNCC2)=NC3=CC=CC=C3C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
DMSO : 8.33 mg/mL (39.06 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 0.83 mg/mL (3.89 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (3.89 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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 (protect from light)
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.
Reinheit & Dokumentation
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Data Sheet (273 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Mok E, et al. Effect of quipazine, a selective 5-HT3 agonist, on dietary self-selection of different macronutrient diets in male and female rats. Appetite. 2000 Jun;34(3):313-25. [Content Brief]
[2]. Günther S, et al. X-ray screening identifies active site and allosteric inhibitors of SARS-CoV-2 main protease. Science. 2021 May 7;372(6542):642-646. [Content Brief]
[3]. Glennon RA, et al. 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80. [Content Brief]
[4]. Ireland SJ, Tyers MB. Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve. Br J Pharmacol. 1987 Jan;90(1):229-38. [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 (protect from light). 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 | 4.6887 mL | 23.4434 mL | 46.8867 mL | 117.2168 mL |
| 5 mM | 0.9377 mL | 4.6887 mL | 9.3773 mL | 23.4434 mL | |
| 10 mM | 0.4689 mL | 2.3443 mL | 4.6887 mL | 11.7217 mL | |
| 15 mM | 0.3126 mL | 1.5629 mL | 3.1258 mL | 7.8145 mL | |
| 20 mM | 0.2344 mL | 1.1722 mL | 2.3443 mL | 5.8608 mL | |
| 25 mM | 0.1875 mL | 0.9377 mL | 1.8755 mL | 4.6887 mL | |
| 30 mM | 0.1563 mL | 0.7814 mL | 1.5629 mL | 3.9072 mL |
Quipazine Related Classifications
HY-W028142 Related Classifications
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