Linagliptin

Linagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4) with an IC50 value of 1 nM for human recombinant DPP-4. It is selective, with >10,000-fold selectivity for DPP-4 over a panel of 11 peptidases and proteases. Linagliptin (3 mg/kg) inhibits 90% of plasma DPP-4 activity in rat. It also dose-dependently decreases plasma glucose and increases plasma levels of glucagon-like peptide 1 (GLP-1) and insulin in Zucker diabetic fatty rats. Oral administration of linagliptin reduces HbA1c levels in mice with high-fat diet- and low-dose streptozotocin-induced diabetes. Formulations containing linagliptin have been used for the treatment of type 2 diabetes mellitus.Formal Name: 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione. CAS Number: 668270-12-0. Synonyms: BI-1356. Molecular Formula: C25H28N8O2. Formula Weight: 472.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 2 mg/ml, Ethanol: 0.2 mg/ml. lambdamax: 203, 226, 293 nm. SMILES: CC1=NC(CN2C(N(C)C(N=C(N3C[C@H](N)CCC3)N4CC#CC)=C4C2=O)=O)=NC5=CC=CC=C51. InChi Code: InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1. InChi Key: LTXREWYXXSTFRX-QGZVFWFLSA-N.