An activator of Ca²⁺ release channel/ryanodine receptors.

33-mer basic peptide cross-linked by three disulphide bridges. Synthetic, from Scorpio maurus palmatus scorpion venom.

• Molecular Weight : 3857.2 Da
  
  
• Solubility in : aqueous solution.
  
  
• Purity min. : >99%
  
  
• Physical Form : white powder
  
  
• Biological Activity : Agonist of ryanodine receptor type 1, 2 and 3 - Potently and reversibly modifies channel gating behaviour of the type 1 ryanodine receptor (RyR1) by inducing increased opening probabilities and a prominent subconductance behaviour.
  
  Binds to a different site than ryanodine.

  Class of biological activity: Ca²⁺ channel activator.
  At cellular level: Myotubes, HEK293 cells expressing RyR1.
  Potency: EC₅₀ at 12 to 20 nM.

  Field of use: Therapeutic potential, notably as candidate immuno-suppressive drugs, and for the treatment of diseases induced by dysfunction of calcium channels, in man.
  Research in pharmacology and physiology.
  
  
• Toxicity (LD₅₀) : Lethal dose: 20 µg/mice (ICV).
  Route of administration: Intracerebroventricular & intravenous.
  
  
• Storage recommendations : Stable at room temperature, store preferably at -20°C.
  
  
• Reconstitution : in aqueous solution.
  
  
• Safety recommendations : Use gloves, wear mask, manipulate under hood.
  
  
• Bibliography :
  
  1. Fajloun Z, Kharrat R, Chen L, Lecomte C, di Luccio E, Bichet D, El Ayeb M, Rochat H, Allen PD, Pessah IN, De Waard, M & Sabatier J-M.Chemical synthesis and characterization of maurocalcine, a scorpion toxin that activates Ca²⁺ release channel / ryanodine receptors. FEBS Letters 469: 179-185 (2000).
  2. Chen L, Estève E, Sabatier JM, Ronjat M, De Waard M, Allen PD & Pessah IN.Maurocalcine and peptide A stabilize distinct subconductance states of ryanodine receptor type 1 (RyR1) revealing a proportional gating mechanism. Journal of Biological Chemistry 278: 16095-16106 (2003).
  3. Estève E, Smida-Rezgui S, Sarkozi S, Szegedi C, Regaya I, Chen L, Altafaj X, Rochat H, Allen P, Pessah IN, Marty I, Sabatier JM, Jona I, De Waard M & Ronjat M.Critical amino acid residues determine the binding affinity and the Ca²⁺ release efficacy of maurocalcine in skeletal muscle cells. Journal of Biological Chemistry 278: 37822-37831 (2003).
  4. Estève E, Mabrouk K, Dupuis A, Smida-Rezgui S, Altafaj X, Grunwald D, Platel JC, Andreotti N, Marty I, Sabatier JM, Ronjat M & De Waard M.Transduction of the scorpion toxin maurocalcine into cells – Evidence that the toxin crosses the plasma membrane. Journal of Biological Chemistry 280: 12833-12839 (2003).
  5. Szappanos H, Smida-Rezgui S, Cseri J, Simut C, Sabatier JM, De Waard M, Kovács L, Csernoch L & Ronjat M.Differential effects of Maurocalcine on Ca²⁺ release events and depolarisation induced Ca²⁺ release in rat skeletal muscle. Journal of Physiology 565: 843-853 (2005).
  6. Boisseau S, Mabrouk K, Garmy N, Collin V, Tadmouri A, Mikati A, Sabatier JM, Ronjat M, Fantini J, De Waard M.Cell penetration properties of maurocalcine, a natural venom peptide active on the intracellular ryanodine receptor. Biochimica Biophysica Acta Biomembranes 1758 : 308-319 (2005).