Linagliptin-d5

Linagliptin-d5 (BI 1356-d5) is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

Product Specifications

Product Name Alternative

BI 1356-d5

UNSPSC

12352005

Target

Autophagy; Dipeptidyl Peptidase; Ferroptosis; Isotope-Labeled Compounds

Related Pathways

Apoptosis; Autophagy; Metabolic Enzyme/Protease; Others

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Smiles

O=C1N(C2=C(C(N1C([2H])([2H])C3=NC(C)=C4C=CC=CC4=N3)=O)N(CC#CC([2H])([2H])[2H])C(N5CCC[C@@H](N)C5)=N2)C

Molecular Formula

C25H23D5N8O2

Molecular Weight

477.57

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Thomas L, et al. (R) -8- (3-amino-piperidin-1-yl) -7-but-2-ynyl-3-methyl-1- (4-methyl-quinazolin-2-ylmethyl) -3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action|[3]Eckhardt M, et al. 8- (3- (R) -aminopiperidin-1-yl) -7-but-2-ynyl-3-methyl-1- (4-methyl-quinazolin-2-ylmethyl) -3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 d|[4]Schurmann C, et al. The dipeptidyl peptidase-4 inhibitor linagliptin attenuates inflammation and accelerates epithelialization in wounds of diabetic ob/ob mice. J Pharmacol Exp Ther. 2012 Jul;342 (1) :71-80.|[5]Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7 (1) :4351.