Teneligliptin (hydrobromide hydrate)

Teneligliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s = 0.37 and 0.29 nM for the human and rat enzymes, respectively). It is selective for DPP-4 over DPP-8 and DPP-9 (IC50s = 260 and 540 nM, respectively, for the human enzymes). Teneligliptin (0.03-1 mg/kg) inhibits increases in plasma glucose levels in an oral glucose tolerance test in Zucker fatty rats. It reduces body weight, inhibits hepatic steatosis, and decreases plasma insulin levels in a mouse model of high-fat diet-induced obesity when administered at doses of 30 and 60 mg/kg. Teneligliptin scavenges hydroxyl radicals in a cell-free assay (IC50 = 0.315 mM) and decreases urinary levels of 8-hydroxy-2'-deoxyguanosine (8-OHdG, Cay-89320), a marker of oxidative stress, in a DPP-4-deficient rat model of diabetes induced by streptozotocin (STZ, Cay-13104) when administered at a dose of 10 mg/kg per day.Formal Name: [(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]-3-thiazolidinyl-methanone, hydrobromide hydrate. CAS Number: 1572583-29-9. Molecular Formula: C22H30N6OS . 2.5HBr [XH2O]. Formula Weight: 426.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 2 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 246 nm. SMILES: CC1=NN(C2=CC=CC=C2)C(N3CCN([C@]4([H])CN[C@H](C(N5CSCC5)=O)C4)CC3)=C1.CC6=NN(C7=CC=CC=C7)C(N8CCN([C@]9([H])CN[C@H](C(N%10CSCC%10)=O)C9)CC8)=C6.Br.Br.Br.Br.Br.O. InChi Code: InChI=1S/8C22H30N6OS.5BrH.H2O/c8*1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27,,,,,,/h8*2-6,13,19-20,23H,7-12,14-16H2,1H3,5*1H,1H2/t8*19-,20-,,,,,,/m00000000....../s1. InChi Key: YTWCZWHMTNJJNO-UHTVBAIESA-N.