1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Cisapride

Cisapride (Synonyms: R 51619; (±)-Cisaprid)

Cat. No.: HY-14149 Purity: 99.72%
Handling Instructions

Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.

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

Cisapride Chemical Structure

Cisapride Chemical Structure

CAS No. : 81098-60-4

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10 mM * 1 mL in DMSO USD 79 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor. IC50 Value: 0.14 μM(EC50 for 5-HT4 receptor) [1]; 9.8 μM (Kv4.3) [2] Target: 5-HT4 Receptor in vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M [1]. cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM [2]. in vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs [3]. cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis[4]. Toxicity: cardiac arrythmies

IC50 & Target

5-HT4 Receptor

0.14 μM (EC50)

Clinical Trial
Molecular Weight

465.95

Formula

C₂₃H₂₉ClFN₃O₄

CAS No.

81098-60-4

SMILES

O=C(N[[email protected]@H]1[[email protected]](OC)CN(CCCOC2=CC=C(F)C=C2)CC1)C3=CC(Cl)=C(N)C=C3OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.62 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1462 mL 10.7308 mL 21.4615 mL
5 mM 0.4292 mL 2.1462 mL 4.2923 mL
10 mM 0.2146 mL 1.0731 mL 2.1462 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: ≥ 2.5 mg/mL (5.37 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

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

CisaprideR 51619 (±)-CisapridR51619R-516195-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Cisapride
Cat. No.:
HY-14149
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