µ-Conotoxin (acetate)

A conotoxin and an inhibitor of Nav1.4 receptors, inhibits Nav1.4 in HEK293 cells (IC50 = 2.3 nM for the rat channel), inhibits rat Nav1.2 channels in HEK293 cells at 500 nM and is an antagonist of a7 nAChRs and a4ß2 and a3ß2 subunit-containing nAChRs in Xenopus oocytes expressing the human receptors (IC50s = 22, 2.9, and 0.45 µM, respectively), reduces global nerve action potential in isolated mouse sciatic nerves in a concentration-dependent manner, inhibits contraction in isolated mouse hemidiaphragm muscles (IC50 = 46 nM). Formulation: A solid. InChI: InChI=1S/C92H139N35O28S6.C2H4O2/c1-43-73(138)113-50(15-8-22-102-91(97)98)79(144)124-64-41-161-160-40-63-88(153)119-55(27-66(95)130)76(141)107-33-70(134)127-24-10-17-65(127)90(155)116-48(13-4-6-20-93)74(139)105-31-68(132)111-60(37-157-156-36-59(72(96)137)123-89(64)154)85(150)122-58(35-129)84(149)121-57(34-128)83(148)114-49(14-5-7-21-94)77(142)117-53(25-44-29-104-47-12-3-2-11-46(44)47)81(146)125-62(39-159-158-38-61(86(151)126-63)112-69(133)32-106-75(140)52-18-19-67(131)110-52)87(152)115-51(16-9-23-103-92(99)100)78(143)120-56(28-71(135)136)82(147)118-54(80(145)109-43)26-45-30-101-42-108-45,1-2(3)4/h2-3,11-12,29-30,42-43,48-65,104,128-129H,4-10,13-28,31-41,93-94H2,1H3,(H2,95,130)(H2,96,137)(H,101,108)(H,105,139)(H,106,140)(H,107,141)(H,109,145)(H,110,131)(H,111,132)(H,112,133)(H,113,138)(H,114,148)(H,115,152)(H,116,155)(H,117,142)(H,118,147)(H,119,153)(H,120,143)(H,121,149)(H,122,150)(H,123,154)(H,124,144)(H,125,146)(H,126,151)(H,135,136)(H4,97,98,102)(H4,99,100,103),1H3,(H,3,4)/t43-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,/m0./s1. InChIKey: FQXXEZBBTACUFG-HJSVBHBKSA-N. SMILES: [H]N([C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@@H](CC(N)=O)C(NCC(N1CCC[C@H]1C(N[C@@H](CCCCN)C(NCC(N[C@H](C(N[C@@H](CO)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@H](C2=O)CC3=CNC4=C3C=CC=C4)=O)=O)=O)=O)CSSC[C@H](N5)C(N)=O)=O)=O)=O)=O)=O)=O)CSSC[C@H](N6)C5=O)=O)CSSC[C@H](N2)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CCCNC(N)=N)C6=O)=O)C)=O)CC7=CN=CN7)=O)CC(O)=O)=O)=O)=O)=O)CC8)C8=O.CC(O)=O