Linagliptin_668270-12-0_DataSheet_MedChemExpress

P d t D t Sh t Product Name:

Linagliptin CAS No.:

668270-12-0Cat. No.:

HY-10284Product Data Sheet

MWt:

472.54Formula:

C25H28N8O2Purity :>98%

Solubility:

DMSO 17 mg/ml; Water <1 mg/ml

Mechanisms:

Biological Activity:

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Pathways:Metabolism/Protease; Target:DPP4

g g y

IC50 value: 1 nM [1]

Target: DPP-4in vitro: Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM) [1]. Linagliptin acts as a competitive inhibitor with a Ki of 1nM, and also shows 10,000-fold more selectivity for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin, and 90-fold more selectivity than

fibroblast activation protein in vitro [2].in vivo: In male Wistar rats, Beagle dogs, and Rhesus monkeys, Linagliptin shows a highly

ffi i l l ti d t t i hibit ti it i t DPP 4b th 70%i hibiti f References:

[1]. 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 4inhibitor for the treatment of type 2diabetes J Med Chem 2007Dec efficacious, long-lasting, and potent inhibitory activity against DPP-4 by more than 70% inhibition for all three species after oral administration of 1 mg/kg. Oral administration of Linagliptin to db/db mice 45 min before an oral glu...

bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J Med Chem. 2007 Dec

27;50(26):6450-3.[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 4inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl

peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.[3]. Schürmann 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;34...

Caution: Not fully tested. For research purposes only

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