ROR Ligand

DP1 peptide is a high-affinity ROR1-binding peptide with a K_d value of 74.9 nM. When labeled with ⁶⁸Ga, DP1 peptide serves as a PET imaging agent, which features rapid tumor uptake, favorable target-to-nontarget ratios in various tumor models, and renal clearance, enabling non-invasive quantitative visualization of ROR1 expression. DP1 peptide can be used in research related to melanoma, hepatocellular carcinoma, colorectal cancer, and non-small cell lung cancer.

Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn²⁺, and 0.88 μM and 0.97 μM in the presence of Zn²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases.

NP1 is a NOTA-chelated linear precursor based on the ROR1-targeting peptide. After labeling with [¹⁸F]AlF, NP1 yields [¹⁸F]AlF-NP1, a PET imaging probe with excellent ROR1 specificity (K_D = 141.7 nM), rapid tumor uptake and high target-to-background ratio, which is suitable for non-invasive visualization of various ROR1-overexpressing tumors.