GPCR/G Protein

Galnon is a selective, non-peptide agonist at the galanin receptors GALR.

Guanabenz (GBZ, GA, Wytensin, Wy-8678) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.

Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.

Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity.

Oxyntomodulin (bovine, porcine), a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist.

Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM).

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.

Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.

Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.

[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats.

Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.

[Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist.

iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 that refers to the use of isoserine instead of serine as first amino acid.

Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes.

AY254 is an analogue of AY77. AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling.

AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.