1. Signaling Pathways
  2. GPCR/G Protein
  3. PACAP Receptor

PACAP Receptor

Pituitary adenylyl cyclase activating polypeptide receptor

Pituitary adenylate cyclase-activating polypeptide (PACAP) is a 38-amino acid, C-terminally alpha-amidated peptide that can be isolated from an ovine hypothalamic extract based on its ability to stimulate cAMP formation in anterior pituitary cells. PACAP belongs to the vasoactive intestinal polypeptide (VIP)-secretin-growth hormone-releasing hormone-glucagon superfamily. The sequence of PACAP has been remarkably well conserved during evolution, from protochordates to mammals. PACAP is widely distributed in the brain and peripheral organs, notably in the endocrine pancreas, gonads, and the respiratory and urogenital tracts. Two types of PACAP binding sites have been characterized: type I binding sites exhibit a high affinity for PACAP and a much lower affinity for VIP, whereas type II binding sites have a similar affinity for both PACAP and VIP.
Molecular cloning of PACAP receptors has shown the existence of three distinct receptor subtypes: the PACAP-specific PAC1-R, which is coupled to several transduction systems, and the PACAP/VIP-indifferent VPAC1-R and VPAC2-R, which are primarily coupled to adenylyl cyclase. PAC1-Rs are particularly abundant in the brain, pituitary, and adrenal gland, whereas VPAC receptors are expressed mainly in the lung, liver, and testis[1].

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P0221
    PACAP (1-38), human, ovine, rat
    99.99%
    PACAP (1-38), human, ovine, rat is a PAC1 receptor agonist. PACAP (1-38), human, ovine, rat binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively. PACAP (1-38), human, ovine, rat increases the α-secretase activity. PACAP (1-38), human, ovine, rat elevates cytosolic Ca2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP (1-38), human, ovine, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP (1-38), human, ovine, rat can be used for neurotrophic and neuroprotective research.
    PACAP (1-38), human, ovine, rat
  • HY-P0220A
    PACAP (6-38), human, ovine, rat TFA
    99.89%
    PACAP (6-38), human, ovine, rat TFA is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
    PACAP (6-38), human, ovine, rat TFA
  • HY-P0176
    PACAP (1-27), human, ovine, rat
    99.30%
    PACAP (1-27), human, ovine, rat (PACAP 1-27) is the N-terminal fragment of PACAP-38, and is a potent PACAP receptor agonist with IC50s of 3 nM, 2 nM and 5 nM for rat PAC1, rat VPAC1 and human VPAC2, respectively.
    PACAP (1-27), human, ovine, rat
  • HY-P0221C
    PACAP (1-38) free acid
    99.94%
    PACAP (1-38) free acid is a desamido-PACAP (1-38), human, ovine, rat (HY-P0221). PACAP (1-38) free acid can activate the human PAC1 receptor. PACAP (1-38) free acid induces cyclic AMP (cAMP) generation in both NS-1 neuroendocrine cells and non-neuroendocrine HEK293 cells.
    PACAP (1-38) free acid
  • HY-P6292A
    KS-133 TFA
    Antagonist 98.95%
    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.
    KS-133 TFA
  • HY-P10768A
    Ro 25-1553 TFA
    Agonist
    Ro 25-1553 TFA is a 31 amino acid vasoactive intestinal peptide (VIP) analog, that acts as an agonist for VIP2 receptor (VPAC2 receptor). Ro 25-1553 TFA exhibits a bronchodilator effect in nerve-induced or Carbachol (HY-B1208)-induced tracheal smooth muscle contraction in guinea pig model.
    Ro 25-1553 TFA
  • HY-P10768B
    Ro 25-1553 acetate
    Agonist
    Ro 25-1553 acetate is a selective VIP2 receptor (VPAC2 receptor) agonist. Ro 25-1553 acetate exhibits bronchodilatory effects on tracheal smooth muscle contractions induced by nerve stimulation or Carbachol (HY-B1208). Ro 25-1553 acetate produces a superimposed effect when combined with Formoterol and Salmeterol (HY-14302). Ro 25-1553 acetate can be used for the study of bronchoconstriction.
    Ro 25-1553 acetate
  • HY-133529
    PA-8
    PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM.
    PA-8
  • HY-147557
    PA-915
    Antagonist 99.17%
    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.
    PA-915
  • HY-P0220
    PACAP (6-38), human, ovine, rat
    99.98%
    PACAP (6-38), human, ovine, rat is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
    PACAP (6-38), human, ovine, rat
  • HY-P4776
    Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27)
    Antagonist 98.01%
    Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27), a vasoactive intestinal peptide (VIP), is a VIP1 antagonist.
    Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27)
  • HY-P2609F
    PACAP (1-38), amide, Biotin-labeled
    98.29%
    PACAP (1-38), amide, Biotin-labeled is a biological active peptide. (Biotin-labeled HY-P0221)
    PACAP (1-38), amide, Biotin-labeled
  • HY-P4127A
    M65 TFA
    Inhibitor 99.98%
    M65 TFA is a deleted peptide of maxadilan (61 a.a.) with deletion of the residues between positions 24 and 42 and is a specific antagonist of PACAP type 1 receptor that inhibits ANP secretion and can be used for relevant researches.
    M65 TFA
  • HY-P0176A
    PACAP (1-27), human, ovine, rat TFA
    99.81%
    PACAP (1-27), human, ovine, rat TFA (PACAP 1-27 TFA) is the N-terminal fragment of PACAP-38, and is a potent PACAP receptor agonist with IC50s of 3 nM, 2 nM and 5 nM for rat PAC1, rat VPAC1 and human VPAC2, respectively.
    PACAP (1-27), human, ovine, rat TFA
  • HY-P1159A
    [D-p-Cl-Phe6,Leu17]-VIP TFA
    98.16%
    [D-p-Cl-Phe6,Leu17]-VIP TFA 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 TFA has no activity on glucagon, secretin or GRF receptors.
    [D-p-Cl-Phe6,Leu17]-VIP TFA
  • HY-P1015
    VIP(Guinea pig)
    Ligand 98.66%
    VIP Guinea pig (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guinea pig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function.
    VIP(Guinea pig)
  • HY-129421
    PA-9
    99.73%
    PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain.
    PA-9
  • HY-P11288A
    ANT308 TFA
    Antagonist 99.57%
    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).
    ANT308 TFA
  • HY-P6292
    KS-133
    Antagonist 98.75%
    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.
    KS-133
  • HY-P990481
    Anti-PACAP38 Antibody
    Anti-PACAP38 Antibody is a human antibody expressed in CHO cells, targeting PACAP38. The Anti-PACAP38 Antibody has a huIgG4SP type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-PACAP38 Antibody can refer to Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-PACAP38 Antibody
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