PACAP Receptor Antagonist

KS-133 TFA is a highly selective and potent antagonist of the vascular active enteropeptide receptor 2 (VIPR2) with IC₅₀ values for Ca influx measurement and cAMP measurement of 24.8 nM and 500 nM, respectively. KS-133 TFA reverses the tumor-promoting M2 phenotype of tumor-associated macrophages to the anti-tumor M1 phenotype, alters the tumor immune microenvironment, and inhibits tumor growth. KS-133 TFA can be used for research on schizophrenia and cancer immune regulation.

PA-915 (PAC1R antagonist 1) is a potent and orally active antagonist of PAC1 receptor. PA-915 inhibits pituitary adenylate cyclase-activating polypeptide (PACAP)-induced CREB phosphorylation. PA-915 can inhibit PACAP- and nerve injury-induced allodynia. PA-915 can be used for the research of neuropathic pain.

Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27), a vasoactive intestinal peptide (VIP), is a VIP₁ antagonist.

ANT308 TFA is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 TFA significantly enhances the activation and proliferation of T cells. ANT308 TFA inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 TFA can be used for the study of acute myeloid leukemia (AML) and uveal melanoma (UVM).

KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer.

ANT308 is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 significantly enhances the activation and proliferation of T cells. ANT308 inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 can be used for the studies of acute myeloid leukemia (AML) and uveal melanoma (UVM).

[D-p-Cl-Phe6,Leu17]-VIP is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC₅₀ of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP has no activity on glucagon, secretin or GRF receptors.