Mambalgin-1 was initially isolated by Sylvie Diochot and collaborators from the venom of the black mamba (Dendroaspis polylepis polylepis). Mambalgin-1 is a potent and selective blocker of acid-sensing ion channels (ASIC). ASIC channels have been demonstrated to be implied in pain pathways and appear to be promising therapeutic targets. Mambalgin-1 rapidly and reversibly inhibits recombinant homomeric ASIC1a (IC50=55 nM) and heteromeric ASIC1a+ASIC2a (IC50=246 nM) or ASIC1a+ASIC2b channels (IC50=61 nM) but also human channels hASIC1b (IC50=192 nM) and hASIC1a+hASIC1b (IC50=72nM). Mambalgin-1 belongs to the family of three-finger toxins and has no sequence/structural homology with either PcTx1 or APETx2. Mambalgin-1 differs from mambalgin-2 by one amino acid. Both have demonstrated a similar activity. Mambalgin-1 has no effect on ASIC2a, ASIC3, ASIC1a+ASIC3 and ASIC1b+ASIC3 channels, as well as on TRPV1, P2X2, 5-HT3A, Nav1.8, Cav3.2 and Kv1.2 channels.
- Applications:TARGET CLASS: ASIC; TARGET: ASIC1; ACTION: Blocker
Peptides & proteins
AA SEQUENCE: LKC3YQHGKVVTC12HRDMKFC19YHNTGMPFRNLKLILQGC37SSSC41SETENNKC49C50STDRC55NK-OH; DISULFIDE BONDS: Cys3-Cys19, Cys12-Cys37, Cys41-Cys49, Cys50-Cys55; SOURCE: synthetic; PURITY: > 98%