TC4

TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC50 values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization) . TC4 can be used for research on obesity and diabetes[1].

12352209

GCGR; GLP Receptor; Neuropeptide Y Receptor

GPCR/G Protein; Neuronal Signaling

Metabolism-protein/nucleotide metabolism

Metabolic Disease

O=C(NC(C)(C)C(N[C@@H](CCC(N)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H]([C@H](O)C)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@@H](CC2=CC=C(C=C2)O)C(N[C@@H](CO)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCNC(CCNC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)C(N[C@@H](C)C(N[C@@H](CCC(N)=O)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC4=CC=C(C=C4)O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCC(O)=O)C(NCC(NCC(N5[C@@H](CCC5)C(N[C@@H](CO)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC6=CNC=N6)C(N[C@@H](CC7=CC=C(C=C7)O)C(N[C@@H](C(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H](CC8=CNC9=CC=CC=C89)C(N[C@@H](CC(C)C)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC%10=CC=C(C=C%10)O)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)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC%11=CC=C(C=C%11)O)N

C277H423N69O78

5967.74

[1]Dinsmore TC, et al. Molecular Design of Unimolecular Tetra-Receptor Agonists. J Am Chem Soc. 2025 Jun 18;147 (24) :20819-20832.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-P11275/

Peptides

No Development Reported