Guangxitoxin 1E (TFA)

Guangxitoxin 1E TFA is the TFA salt form of Guangxitoxin 1E (HY-P1427). Guangxitoxin 1E TFA is a peptide toxin and a selective inhibitor for voltage-gated potassium channel KV2.1 and KV2.2 with IC50 of 1-3 nM. Guangxitoxin 1E TFA enhances glucose-stimulated intracellular calcium ion oscillations and increases insulin secretion in a glucose-dependent manner[1].

O=C(NCC(N[C@@H](CCC(O)=O)C(N[C@@H](CSSC[C@@H](C(N1[C@@H](CCC1)C(N[C@@H](CCCCN)C(N[C@@H](CC2=CC=C(C=C2)O)C(N[C@H]3C(C)C)=O)=O)=O)=O)NC4=O)C(NCC(NCC(N[C@@H](CC5=CC=CC=C5)C(N[C@@H](CC6=CNC7=CC=CC=C67)C(N[C@@H](CC8=CNC9=CC=CC=C89)C(N[C@@H](CCCCN)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CO)C(N%10[C@@H](CCC%10)C(N[C@@H](CCCCN)C(N[C@@H](CC(/C%11=C/C)=CNC%11=C)C(NCC(N[C@H]%12CC(C)C)=O)=O)=O)=O)=O)=O)NC3=O)C(NCC(N[C@@H](CO)C(NCC(N[C@@H](CCCCN)C(N%13[C@@H](CCC%13)C(N[C@@H](C)C(N[C@H]4CSSC[C@@H](C(N[C@@H](CC(N)=O)C(N[C@@H](CC%14=CC=CC=C%14)C(N%15[C@@H](CCC%15)C(N[C@@H](CCSC)C(N%16[C@@H](CCC%16)C(O)=O)=O)=O)=O)=O)=O)NC%12=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCC(O)=O)N.OC(C(F)(F)F)=O.[x]

[1]Herrington J, et al. Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-dependent insulin secretion. Diabetes. 2006 Apr;55(4):1034-42.