Pentagastrin

Pentagastrin is a synthetic polypeptide and cholecystokinin-2 (CCK2) receptor agonist. It binds selectively to CCK2 receptors in guinea pig brain over CCK1 receptors in rat pancreas (IC50s = 11 and 1,100 nM, respectively). Pentagastrin increases calcium influx and polyphosphoinositide turnover in rat GH3 pituitary cells (EC50s = 23 and 3.9 nM, respectively). It also increases histidine decarboxylase activity in mucous- and endocrine cell-enriched isolated rabbit fundic mucosal cells (EC50 = 2.9 nM). Pentagastrin induces contraction of isolated pig ileum smooth muscle cells in vitro (EC50 = 30 pM). It increases gastric acid and pepsin secretion in conscious cats in vivo (ED50s = 1.29 and 57.3 nmol/kg2 per hour, respectively). Formulations containing pentagastrin have previously been used as a diagnostic aid to evaluate gastric acid secretory function.Formal Name: N-[(1,1-dimethylethoxy)carbonyl]-beta-alanyl-L-tryptophyl-L-methionyl-L-alpha-aspartyl-L-phenylalaninamide. CAS Number: 5534-95-2. Synonyms: AY 6608, NSC 367746. Molecular Formula: C37H49N7O9S. Formula Weight: 767.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25 mg/ml, DMSO: 20 mg/ml, Ethanol: 0.3 mg/ml, PBS (pH 7.2): 0.5 mg/ml. lambdamax: 220, 283 nm. SMILES: CC(C)(C)OC(NCCC(N[C@@H](CC1=CC2=C(C=CC=C2)N1)C(N[C@@H](CCSC)C(N[C@@H](CC(O)=O)C(N[C@@H](CC3=CC=CC=C3)C(N)=O)=O)=O)=O)=O)=O. InChi Code: InChI=1S/C37H49N7O9S/c1-37(2,3)53-36(52)39-16-14-30(45)41-28(20-24-19-23-12-8-9-13-25(23)40-24)34(50)42-26(15-17-54-4)33(49)44-29(21-31(46)47)35(51)43-27(32(38)48)18-22-10-6-5-7-11-22/h5-13,19,26-29,40H,14-18,20-21H2,1-4H3,(H2,38,48)(H,39,52)(H,41,45)(H,42,50)(H,43,51)(H,44,49)(H,46,47)/t26-,27-,28-,29-/m0/s1. InChi Key: XFMFMOVRGXQQHB-DZUOILHNSA-N.