Calciseptine (TFA)

Calciseptine TFA is a natural peptide toxin found in the venom of the black mamba snake (Dendroaspis p. polylepis) . Calciseptine TFA is a highly effective and selective blocker of the L-type channel of the Cav1.2 subtype, with an IC50 value of 92 nM. Calciseptine TFA has no effect on Cav3.1, Cav2.2, Cav2.1, Cav1.1, voltage-sensitive sodium channels and potassium channels. Calciseptine TFA has negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine TFA can be used for the study of cardiovascular diseases[1].

12352209

Calcium Channel

Membrane Transporter/Ion Channel; Neuronal Signaling

Cardiovascular Disease

O=C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CC1=CC=C(C=C1)O)C(N[C@@H](CCCCN)C(N[C@@H](CCSC)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCCNC(N)=N)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC3=CC=C(C=C3)O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CO)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCCNC(N)=N)C(NC4)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC5=O)C(N[C@@H](CC6=CC=C(C=C6)O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC7=CNC=N7)C(N[C@@H](CCCCN)C(N[C@@H](C)C(N[C@@H](CO)C(N[C@@H](CC(C)C)C(N8[C@@H](CCC8)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCCCN)C(N[C@@H]([C@H](O)C)C(N[C@@H](CSSC[C@@H](C(NCC(N[C@@H](CSSC[C@@H](C(N[C@@H](CSSC[C@@H](C(N[C@@H](CC(N)=O)C(N[C@@H](CCCCN)C(O)=O)=O)=O)NC9=O)C(N[C@@H](CCCCN)C(NCC(N[C@@H](CC(O)=O)C(N[C@H]9CCCNC(N)=N)=O)=O)=O)=O)=O)NC%10=O)C(N%11[C@@H](CCC%11)C(N[C@@H]([C@H](O)C)C(N[C@@H](C)C(N[C@@H](CCSC)C(N[C@@H](CC%12=CNC%13=CC=CC=C%12%13)C(N%14[C@@H](CCC%14)C(N[C@@H](CC%15=CC=C(C=C%15)O)C(N[C@@H](CCC(N)=O)C(N[C@@H]([C@H](O)C)C(N[C@H]%10CCC(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC4=O)C(N[C@@H](C(C)C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC(N)=O)C(N[C@H]5[C@H](O)C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCCNC(N)=N)N.O=C(O)C(F)(F)F.[x]

C299H468N90O87S10.xC2HF3O2

7036.12 (free base)

[1]Mesirca P, et al. Selective blockade of Cav1.2 (α1C) versus Cav1.3 (α1D) L-type calcium channels by the black mamba toxin calciseptine. Nat Commun. 2024 Jan 2;15 (1) :54.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-P3269A/

Peptides

No Development Reported

L-type calcium channel