Peptide Conjugates

TATE-DA-I is a somatostatin receptor 2 (SSTR2) ligand with an IC₅₀ of 25.3 nM. TATE-DA-I binds to albumin to prolong its circulation retention time and also exhibits enhanced tumor accumulation capacity. TATE-DA-I enables clear visualization of SSTR2-positive tumors in SPECT/CT imaging. TATE-DA-I can be used in cancer-related research.

PSMA-HK9 is a ligand targeting prostate-specific membrane antigen (PSMA) that binds to PSMA with high affinity, with a K_d value of 4.76 nM. PSMA-HK9 can be labeled with the diagnostic radionuclide 68Ga for imaging applications, and this labeled conjugate exhibits high tumor uptake and low normal tissue uptake in vivo. PSMA-HK9 can be labeled with the radionuclide 177Lu for targeted radionuclide studies, and this labeled conjugate possesses efficient cellular endocytosis and tumor inhibitory activity. PSMA-HK9 can be used in studies related to prostate cancer.

Oxoreotide atexetan citrate is a conjugate of a SSTR-targeting peptide and atexetan. Oxoreotide atexetan citrate is used in combination with radioisotopes such as lead-212 (²¹²Pb) to study somatostatin receptor-expressing neuroendocrine tumors (NETs).

Zaregreptide dizuxetan is a SSTR-targeting peptide-DOTA variant conjugate. Zaregreptide dizuxetan can be conjugated with ¹⁷⁷Lutetium for the study of SSTR-positive neuroendocrine tumors.

GALA-chol is a cholesterol-conjugated pH-responsive fusion peptide that can serve as a delivery adjuvant. GALA-chol enhances the endocytosis of siRNA RET/PTC1-SQ nanoparticles, inhibits cell viability, and undergoes pH-responsive charge conversion in the acidic lysosomal environment, thereby promoting lysosomal escape of small extracellular vesicle (sEV) cargo. GALA-chol anchors to the sEV membrane and maintains the structural integrity and intrinsic homing activity of sEVs. GALA-chol can be used in studies related to adjuvant delivery.

LF1 is a gastrin-releasing peptide receptor (GRPR) antagonist. LF1 can be stably radiolabeled with gallium-⁶⁸, indium-¹¹¹, and lutetium-¹⁷⁷. Radiolabeled LF1 can be used for high-contrast SPECT/CT imaging. LF1 is applicable to prostate cancer-related research.

Ac-crown-TATE is an actinium-labeled radioligand derived from the SSTR2 agonist crown-TATE, which targets neuroendocrine tumors with high SSTR2 expression. The [226Ac]Ac-crown-TATE form of Ac-crown-TATE possesses both SPECT-detectable γ-emission and α-radiation properties, and it inhibits tumor growth and prolongs survival. Ac-crown-TATE can be used in studies of SSTR2-positive neuroendocrine tumors, targeted α-radiation, and radionuclide imaging.

Granzyme B contrast agent-1 is a Granzyme B binder with a K_d value of 1.0 nM. When radiolabeled, Granzyme B contrast agent-1 can be used for positron emission tomography (PET) and single-photon emission computed tomography (SPECT) imaging studies of Granzyme B.

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.

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.

AT1R-agonist-1 is an angiotensin II type 1 receptor (AT1R) agonist with a K_i value of 1.4 nM. AT1R-agonist-1 exhibits low Gαq activity, retains β-arrestin recruitment function, and accesses the deep allosteric pocket inside AT1R via its flexible side chain. AT1R-agonist-1 possesses positive inotropic effects (enhancing cardiac contractile function) and causes almost no increase in blood pressure. AT1R-agonist-1 can be used for research on conditions such as refractory cardiogenic shock.

DOTA-cTMTP1 is a cyclic tumor-homing peptide precursor molecule. DOTA-cTMTP1 selectively binds to XPNPEP2 on highly metastatic tumor cells, accumulates and retains in hepatocellular carcinoma tumors, and maintains a high tumor-to-liver contrast over time in small animal models. After radiolabeling with ⁶⁸Ga, DOTA-cTMTP1 forms a PET probe for positron emission tomography (PET) imaging of hepatocellular carcinoma (HCC).

DOTA-TH10 is a CSPG4-targeted probe that enables targeted enrichment in tumors with overexpressed CSPG4. ⁶⁸Ga-radiolabeled DOTA-TH10 specifically binds to CSPG4, allowing visualization of CSPG4 expression. ⁶⁸Ga-radiolabeled DOTA-TH10 exhibits significant tumor uptake capacity in pancreatic cancer and gastric cancer models. DOTA-TH10 can be used for research on pancreatic cancer and gastric cancer.

ADA2 is an ADAMTS4-binding peptide and imaging agent with a human ADAMTS4 K_a of 5.3 nM and reduced renal uptake compared to related tracers. ADA2 accumulates in dilated aortic regions in aortic aneurysm mouse models. ADA2 exhibits an in vivo safety profile. ADA2 can be used for the research of aortic aneurysm.

NECT-224 is a bifunctional chelator and a nectin-4 targeting peptide conjugate. NECT-224 can be used as a PET imaging agent when labeled with ⁶⁴Cu or ⁶⁸Ga.

DOTA-NT-20.3-IPBA is a Neurotensin receptor 1 (NTR1)-targeting albumin binder with specific high-affinity binding to NTR1. DOTA-NT-20.3-IPBA is formed by the conjugation of DOTA-NT-20.3 and IPBA. DOTA-NT-20.3-IPBA can be used for positron emission tomography (PET) imaging following labeling with [⁶⁸Ga]Ga.

HYNIC-H10F is a conjugate of HER2-targeting peptide H10F and bifunctional chelator HYNIC. HYNIC-H10F can be used in breast cancer-related research.

HYNIC-H6F is a SPECT imaging probe with binding specificity for human epidermal growth factor receptor 2 (HER2) domain II (IC₅₀ = 11 nM). HYNIC-H6F accumulates in HER2-positive breast cancer xenografts via receptor-mediated uptake, while shows low uptake in HER2-negative breast cancer xenografts. HYNIC-H6F enables non-invasive detection of HER2-positive breast cancer in mouse models and allows evaluation of HER2 expression levels without blocking interference. HYNIC-H6F can be used in breast cancer-related research.

10P3Me is a Glypican-3 (GPC3)-targeting probe with a K_a of 93.8 nM for the human target. 10P3Me exhibits high binding affinity to GPC3, targets GPC3-positive cells, and serves as an agent for PET imaging. 10P3Me selectively accumulates in GPC3-positive tumor tissues, including subcutaneous xenograft models and orthotopic HepG2-LUC liver cancer models, to achieve precise localization of lesions.

LCA-H10 is a lithocholic acid-histidine decapeptide conjugate, a biocompatible lipid nanoparticle (LNP) additive that reduces ionizable lipid proportions, functions as an endosomal escape inducer, and enhances siRNA encapsulation. LCA-H10 increases hepatic accumulation of LNPs in mice after intravenous injection when incorporated into LiLNP-LH and reduces proinflammatory cytokines (IL-6, TNF, IL-1β) in mouse serum. LCA-H10 can be used for the research of prostate cancer.