Linagliptin-d4

Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[2140263-92-7]

Product Name Alternative

BI 1356-d4

UNSPSC

12352005

Target

Autophagy; Dipeptidyl Peptidase; Ferroptosis

Type

Isotope-Labeled Compounds

Related Pathways

Apoptosis; Autophagy; Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Purity

99.9

Solubility

10 mM in DMSO|DMSO : 25mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

CC#CCN1C2=C(N(C(N(C2=O)CC3=NC4=C(C=CC=C4)C(C)=N3)=O)C)N=C1N5C([2H])([2H])[C@@H](CCC5([2H])[2H])N

Molecular Formula

C25H24D4N8O2

Molecular Weight

476.57

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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|[3]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.|[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]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