1. GPCR/G Protein
    Neuronal Signaling
    Anti-infection
  2. 5-HT Receptor
    Influenza Virus
  3. Cinanserin hydrochloride

Cinanserin hydrochloride (Synonyms: SQ 10643)

Cat. No.: HY-100943 Purity: 99.74%
Handling Instructions

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.

For research use only. We do not sell to patients.

Cinanserin hydrochloride Chemical Structure

Cinanserin hydrochloride Chemical Structure

CAS No. : 54-84-2

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Description

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[1][2][3].

IC50 & Target[1][3]

5-HT2 Receptor

41 nM (Ki)

3C-like proteinase

 

In Vitro

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].

In Vivo

Cinanserin (5 mg/kg; intravenous injection; for 2 hours; male Wistar rats) treatment significantly reduces systemic burn edema to shamburn levels. Leukocyte-endothelial interactions are significantly reduced by administration of Cinanserin[2].

Animal Model: Male Wistar rats (250 g) underwent thermal injury[2]
Dosage: 5 mg/kg
Administration: Intravenous injection; for 2 hours
Result: Significantly reduced systemic burn edema to shamburn levels..
Molecular Weight

376.94

Formula

C₂₀H₂₅ClN₂OS

CAS No.

54-84-2

SMILES

O=C(NC1=CC=CC=C1SCCCN(C)C)/C=C/C2=CC=CC=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

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
In Vitro: 

DMSO : 125 mg/mL (331.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6529 mL 13.2647 mL 26.5294 mL
5 mM 0.5306 mL 2.6529 mL 5.3059 mL
10 mM 0.2653 mL 1.3265 mL 2.6529 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

CinanserinSQ 10643SQ10643SQ-106435-HT ReceptorInfluenza VirusSerotonin Receptor5-hydroxytryptamine Receptor5-HT2burnsystemicedemaleukocyteendothelial3C-likeproteinasevirusreplicationInhibitorinhibitorinhibit

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Cinanserin hydrochloride
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