pac1

PAC-1 (Procaspase activating compound 1) has been used in trials studying the treatment of Lymphoma, Melanoma, Solid Tumors, Breast Cancer, and Thoracic Cancers, among others.

PAC1R antagonist 1 is an orally active PAC1 receptor antagonist that inhibits abnormal pain induced by pituitary adenylate cyclase-activating polypeptide (PACAP) and nerve damage, and may be used in the study of neoplasms and immune-related disorders.

MK 0893 is a potent and selective Glucagon Receptor (GR) antagonist (IC50=6.6 nM) with competitive, reversible, high binding affinity and functional cAMP activity, which attenuates glucagon induced blood glucose elevation and reduces ambient glucose levels in acute and chronic mouse models.

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

PA-9 is the first small-molecule PAC1 receptor antagonist.

VU0652925 is a PAR4 antagonist. VU0652925 has a P-sel IC50 of 39.2 pM (-pIC50±SEM: 10.41±0.04) and a PAC1 IC50 of 43.0 pM (-pIC50±SEM: 10.4±0.04).

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo.

M65 is a PAC1 receptor-specific antagonist that inhibits the secretion of atrial natriuretic peptide (ANP) [1].

PACAP (1-27), human, ovine, rat TFA (PACAP 1-27 TFA), an N-terminal fragment of PACAP-38, is an effective PACAP receptor antagonist with IC50 values of 3 nM for rat PAC1, 2 nM for rat VPAC1, and 5 nM for human VPAC2.

PACAP-38 (31-38), human, mouse, rat acetate is an activator of PAC1 receptor. PACAP-38 (31-38), human, mouse, rat acetate demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production and can

PACAP (1-38), human, ovine, rat (Pituitary Adenylate Cyclase Activating Polypeptide 38), is a neuropeptide comprising 38 amino acid residues.

Selective VPAC2 receptor agonist (EC50 values are 0.4, 100 and >1000 nM for VPAC2, VPAC1 and PAC1, respectively in a cAMP accumulation assay; IC50 values are 60, 8700 and >10000 nM for VPAC2, VPAC1 and PAC1, respectively in a competition binding assay). S