CH 275 (acetate)

CH 275 is a cyclic peptide agonist of somatostatin receptor 1 (SST1, IC50 = 30.9 nM for the human receptor). It is selective for SST1 over SST2, SST3, SST4, and SST5 (IC50s = >10,000, 345, >1,000, and >10,000 nM, respectively, for the human receptors). CH 275 (500 nM) inhibits basal growth hormone secretion from primary mouse pituitary cells. It inhibits glucose-induced increases in electrical activity without inducing membrane hyperpolarization in a whole-cell patch-clamp assay using MIN6 pancreatic beta-cells when used at a concentration of 100 nM.Formal Name: L-cysteinyl-L-lysyl-L-phenylalanyl-L-phenylalanyl-D-tryptophyl-4-[[(1-methylethyl)amino]methyl]-L-phenylalanyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-cysteine, cyclic (1->11)-disulfide, acetate. Molecular Formula: C74H96N14O15S2 . XC2H4O2. Formula Weight: 1485.8. Purity: >95%. Formulation: (Request formulation change), A solid. Peptide Sequence: CLFFwXTFTSC-OH (X= 4-(N-isopropyl)-aminomethylphenylalanine). Solubility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml, DMSO: Sparingly Soluble: 1-10 mg/ml, Water: Slightly Soluble: 0.1-1 mg/ml. SMILES: [H][C@@]([C@@H](C)O)(NC([C@@H](N1)CC2=CC=C(CNC(C)C)C=C2)=O)C(N[C@@H](CC3=CC=CC=C3)C(N[C@](C(N[C@@H](CO)C(N[C@H](C(O)=O)CSSC[C@H](N)C(N[C@@H](CCCCN)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](CC5=CC=CC=C5)C(N[C@H](CC6=CNC7=CC=CC=C76)C1=O)=O)=O)=O)=O)=O)=O)([C@@H](C)O)[H])=O)=O.CC(O)=O. InChi Code: InChI=1S/C74H96N14O15S2.C2H4O2/c1-42(2)77-37-49-29-27-48(28-30-49)35-57-69(97)87-62(43(3)90)72(100)84-58(34-47-22-12-7-13-23-47)70(98)88-63(44(4)91)73(101)85-60(39-89)71(99)86-61(74(102)103)41-105-104-40-52(76)64(92)79-54(26-16-17-31-75)65(93)80-55(32-45-18-8-5-9-19-45)66(94)81-56(33-46-20-10-6-11-21-46)67(95)83-59(68(96)82-57)36-50-38-78-53-25-15-14-24-51(50)53,1-2(3)4/h5-15,18-25,27-30,38,42-44,52,54-63,77-78,89-91H,16-17,26,31-37,39-41,75-76H2,1-4H3,(H,79,92)(H,80,93)(H,81,94)(H,82,96)(H,83,95)(H,84,100)(H,85,101)(H,86,99)(H,87,97)(H,88,98)(H,102,103),1H3,(H,3,4)/t43-,44-,52+,54+,55+,56+,57+,58+,59-,60+,61+,62+,63+,/m1./s1. InChi Key: LYJPJJXHWZLAIH-UPSMQBAUSA-N.