Description
A peptide class E/R-type calcium channel blocker (IC50 = 30 nM in 192C cells expressing human class E channels); selective for class E/R-type over class A and class B calcium channels (IC50s = >280 and ~800 nM, respectively), as well as the voltage-gated potassium channels Kv1.1, Kv1.2, and Kv1.4 (IC50s = >140 nM for all); inhibits class E/R-type calcium currents in isolated rat posterior pituitary (IC50 = 4 nM); intrathecal administration inhibits formalin-induced NK1 receptor internalization and cfos expression in the ipsilateral dorsal horn and reduces formalin-induced paw flinching in rats at 0.5 µg/animal
Formal name: glycyl-L-valyl-L-α-aspartyl-L-lysyl-L-alanylglycyl-L-cysteinyl-L-arginyl-L-tyrosyl-L-methionyl-L-phenylalanylglycylglycyl-L-cysteinyl-L-seryl-L-valyl-L-asparaginyl-L-α-aspartyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-prolyl-L-arginyl-L-leucylglycyl-L-cysteinyl-L-histidyl-L-seryl-L-leucyl-L-phenylalanyl-L-seryl-L-tyrosyl-L-cysteinyl-L-alanyl-L-tryptophyl-L-α-aspartyl-L-leucyl-L-threonyl-L-phenylalanyl-L-seryl-L-aspartic acid, cyclic (7→21),(14→26),(20→33)-tris(disulfide)
Synonyms:
Molecular weight: 4,495.00
CAS: 203460-30-4
Purity: ≥98%
Formulation: A solid
