Cinanserin hydrochloride
Based on 1 publication(s) in Google Scholar
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
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- Purity: 99.48%
- CAS No.: 54-84-2
- 화학식: C20H25ClN2OS
- 분자량:376.94
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Cinanserin hydrochloride
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT2 Receptor 41 nM (Ki) |
3C-like proteinase |
Cinanserin/Cinanserin hydrochloride have binding affinity to SARS-CoV 3CLpro, HCoV-229E 3CLpro, with the KD values of 49.4 μM/78.0 μM for SARS-associated coronavirus (SARS-CoV) 3CLpro and 18.2 μM/36.6 μM for human coronavirus 229E (HCoV-229E) 3CLpro[1].
The IC50 values of Cinanserin and Cinanserin hydrochloride for inhibiting the catalytic activity of SARS-CoV 3CLpro are calculated as 4.92 μM and 5.05 μM, respectively, The corresponding IC50 values for HCoV-229E 3CLpro are 4.68 μM and 5.68 μM. None of the compounds have inhibitory activity against HRV-14 3Cpro at concentrations up to 200 μM[1].
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:Male Wistar rats (250 g) underwent thermal injury[2]
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Dosage:5 mg/kg
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Administration:Intravenous injection; for 2 hours
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Result:Significantly reduced systemic burn edema to shamburn levels..
Chemical Information
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CAS No. 54-84-2
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Appearance Solid
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분자량 376.94
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화학식 C20H25ClN2OS
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=CC=C1SCCCN(C)C)/C=C/C2=CC=CC=C2.[H]Cl
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Synonyms
SQ 10643
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Rep
Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]2022 Jul 16;12(1):12197. PMID: 35842458
용액&용해도
DMSO : 125 mg/mL (331.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (265.29 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (5.52 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 (5.52 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- 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)
References
[1]. Chen L, et al. Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro. J Virol. 2005 Jun;79(11):7095-103. [Content Brief]
[2]. Hernekamp JF, et al. Cinanserin reduces plasma extravasation after burn plasma transfer in rats. Burns. 2013 Sep;39(6):1226-33. [Content Brief]
[3]. Leysen JE, et al. Receptor binding profile of R 41 468, a novel antagonist at 5-HT2 receptors. Life Sci. 1981 Mar 2;28(9):1015-22. [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 (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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.6529 mL | 13.2647 mL | 26.5294 mL | 66.3236 mL |
| 5 mM | 0.5306 mL | 2.6529 mL | 5.3059 mL | 13.2647 mL | |
| 10 mM | 0.2653 mL | 1.3265 mL | 2.6529 mL | 6.6324 mL | |
| 15 mM | 0.1769 mL | 0.8843 mL | 1.7686 mL | 4.4216 mL | |
| 20 mM | 0.1326 mL | 0.6632 mL | 1.3265 mL | 3.3162 mL | |
| 25 mM | 0.1061 mL | 0.5306 mL | 1.0612 mL | 2.6529 mL | |
| 30 mM | 0.0884 mL | 0.4422 mL | 0.8843 mL | 2.2108 mL | |
| 40 mM | 0.0663 mL | 0.3316 mL | 0.6632 mL | 1.6581 mL | |
| 50 mM | 0.0531 mL | 0.2653 mL | 0.5306 mL | 1.3265 mL | |
| 60 mM | 0.0442 mL | 0.2211 mL | 0.4422 mL | 1.1054 mL | |
| 80 mM | 0.0332 mL | 0.1658 mL | 0.3316 mL | 0.8290 mL | |
| 100 mM | 0.0265 mL | 0.1326 mL | 0.2653 mL | 0.6632 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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