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
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.

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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

Ki: 41 nM (5-HT2 receptor)[3];
3C-like proteinase[1]

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

Please store the product under the recommended conditions in the Certificate of Analysis.

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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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