1. Cytoskeleton
  2. Gap Junction Protein
  3. Rotigaptide

Rotigaptide (Synonyms: ZP123)

Cat. No.: HY-106225 Purity: 99.63%
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Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.

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

Rotigaptide Chemical Structure

Rotigaptide Chemical Structure

CAS No. : 355151-12-1

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10 mM * 1 mL in DMSO USD 611 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation[1][2].

IC50 & Target

IC50: connexin 43 (Cx43)[1]

In Vitro

Rotigaptide (100 nM; 24 hours) has a positive effect on cycloheximide-mediated decrease in Cx43 protein levels in cultured neonatal ventricular myocytes[1].
Rotigaptide (100 nM; 24 hours) dose not affect INS-1 cell apoptosis itself. And it significantly reduces apoptosis in cytokine-exposed cells ~10% at IL-1b concentrations above 15 pg/ml in rat insulin-producing INS-1 cells[2].

Western Blot Analysis[1]

Cell Line: Neonatal cardiomyocytes
Concentration: 100 nM
Incubation Time: 24 hours
Result: Partially prevented the loss of Cx43 protein expression in neonatal cardiomyocytes.

Apoptosis Analysis[2]

Cell Line: Cx43 deficient INS-1 cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Ameliorated cytokine-induced apoptosis associated with improved mitochondrial function.
In Vivo

Rotigaptide (intravenous administration; 300 mg/kg; single dose) treatment in mice and rats does not result in toxicity in either species.
In escalating dose studies, Rotigaptide (continuous intravenous infusion; 5-14 days) in rats (100 mg/kg) and dogs (10 mg/kg) are well tolerated and produces no compound-related effects or histological toxicological findings[3].

Molecular Weight

617.65

Formula

C₂₈H₃₉N₇O₉

CAS No.

355151-12-1

SMILES

O=C(N)CNC([[email protected]@H](C)NC(CNC([[email protected]@H]1N(C([[email protected]@H]2N(C([[email protected]@H](CC3=CC=C(O)C=C3)NC(C)=O)=O)CCC2)=O)C[[email protected]@H](O)C1)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

RotigaptideZP123ZP 123ZP-123Gap Junction Proteincardiacarrhythmiasatrialfibrillatiogapjunction anti‐arrhythmicpeptideInhibitorinhibitorinhibit

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