Tyr-α-CGRP (human) (TFA)

Tyr-α-CGRP (human) TFA is an N-terminally extended human α-CGRP analog. Tyr-α-CGRP (human) TFA can bind to membrane preparations from rat brain and spleen with IC50 values of 0.2 nM and 0.5 nM, respectively, and induce positive chronotropic and inotropic effects in isolated guinea pig right and left atria with EC50 values of 282 nM and 74 nM, respectively. Tyr-α-CGRP (human) TFA also inhibits contractile responses in rat vas deferens with an EC50 value of 1.9 nM[1][2].

O=C(N[C@@H](C)C(N[C@@H](CSSC[C@@H](C(N[C@@H](C(C)C)C(N[C@@H]([C@H](O)C)C(N[C@@H](CC1=CNC=N1)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(NCC(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CO)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CO)C(NCC(NCC(N[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CC(N)=O)C(N[C@@H](CC(N)=O)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H](C(C)C)C(N3[C@@H](CCC3)C(N[C@@H]([C@H](O)C)C(N[C@@H](CC(N)=O)C(N[C@@H](C(C)C)C(NCC(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](C)C(N[C@@H](CC4=CC=CC=C4)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC5=O)C(N[C@@H](CC(O)=O)C(N[C@@H]([C@H](O)C)C(N[C@@H](C)C(N[C@H]5[C@H](O)C)=O)=O)=O)=O)=O)[C@H](CC6=CC=C(C=C6)O)N.OC(C(F)(F)F)=O.[x]

[1]Poyner D R, et al. Pharmacological characterization of a receptor for calcitonin gene‐related peptide on rat, L6 myocytes[J]. British journal of pharmacology, 1992, 105(2): 441-447.|[2]Dennis T, et al. Structure-activity profile of calcitonin gene-related peptide in peripheral and brain tissues. Evidence for receptor multiplicity[J]. Journal of Pharmacology and Experimental Therapeutics, 1989, 251(2): 718-725.