ASIC1a & 1b channel blocker
酸敏感离子通道ASIC1a & 1b通道阻断剂
Mambalgin-1 was initially isolated by Sylvie Diochot and collaborators from the venom of the black mamba (Dendroaspis polylepis polylepis). 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. 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).
belongs to the family of three-finger toxins and has no sequence/structural homology with either PcTx1 or APETx2. differs from mambalgin-2 by one amino acid. Both have demonstrated a similar activity. 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.
Fig 1: Dose-response curve of the effect of synthetic #MAM001 on ASIC1a current recorded in Xenopus oocytes. In this system, an IC50 of 21 nM was determined.
二硫键：Cys3-Cys19, Cys12-Cys37, Cys41-Cys49, Cys50-Cys55
长度 (aa)： 57
外观：White lyophilized solid
可溶性：water or saline buffer
CAS 号：not available