| Description | Rotigaptide is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. |
| In vitro | Rotigaptide (100 nM; 24 hours) does not affect INS-1 cell apoptosis itself. Rotigaptide (100 nM; 24 hours) has a positive effect on the cycloheximide-mediated decrease in Cx43 protein levels in cultured neonatal ventricular myocytes. And it obviously decreases apoptosis in cytokine-exposed cells ~10% at IL-1b concentrations above 15 pg/ml in rat insulin-producing INS-1 cells [1][2]. |
| In vivo | Rotigaptide (intravenous administration; 300 mg/kg; single dose) treatment in mice and rats does not cause toxicity in either species. Rotigaptide (continuous intravenous infusion; 5-14 days) in rats (100 mg/kg) and dogs (10 mg/kg) is well tolerated and produces no compound-related effects or histological toxicological findings in escalating dose studies [3]. |
| Synonyms | ZP123 |
| molecular weight | 617.65 |
| Molecular formula | C28H39N7O9 |
| CAS | 355151-12-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Seyed Mojtaba Ghiasi, et al. The connexin 43 regulator Rotigaptide reduces cytokine-induced cell death in human islets 2. Stahlhut M, et al. The antiarrhythmic peptide rotigaptide (ZP123) increases connexin 43 protein expression in neonatal rat ventricular cardiomyocytes.Cell Commun Adhes. 2006 Jan-Apr;13(1-2):21-7. 3. Kjølbye AL, et al. Pharmacological modulation of gap junction function with the novel compound rotigaptide: a promising new principle for prevention of arrhythmias.Basic Clin Pharmacol Toxicol. 2007 Oct;101(4):215-30. |