Linagliptin Inhibitor CAS No. 668270-12-0

Cat. No.	Name	Size	Price
KI0591	Linagliptin	5 mg	$272
	Linagliptin	10 mg	$432
	Linagliptin	100 mg	$2992
	Linagliptin	200 mg	$4432

Chemical Characteristic

Product Name	Linagliptin
Synonyms	BI-1356, Tradjenta, and Trajenta
CAS No.	668270-12-0
Molecular Weight	472.54
Formula	C₂₅H₂₈N₈O₂
Chemical Name	8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione
Smiles	n1(c(nc2n(c(=O)n(c(=O)c12)Cc1nc2c(c(n1)C)cccc2)C)N1C[C@H](CCC1)N)CC#CC
Chemical Structure
Documents	HPLC MS COA

Biological activities

Linagliptin is a highly potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 of 1 nM. Linagliptin is a competitive inhibitor with a Ki of 1 nM. Linagliptin has about 10,000-fold more selective for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin. Linagliptin has 90-fold more selective than for fibroblast activation protein in vitro.^[1] Linagliptin inhibits transcellular transport of digoxin by P-gp with an apparent IC50 of 66.1 μM. Linagliptin also shows inhibitory potency against organic cation transporter 1 (OCT1) and OCT2.^[2] In HanWistar rats, administration of linagliptin shows more profound DPP-4 inhibition than any of the other DPP-4 inhibitors (including saxagliptin, alogliptin, vildagliptin, and sitagliptin). In C57BL/6J mice and Zucker fatty (fa/fa) rats, the duration of action on glucose tolerance decreases in the order linagliptin > (sitagliptin/saxagliptin) > vildagliptin.^[1] In vivo, linagliptin treatment also attenuates inflammation and accelerates epithelialization in wounds of diabetic ob/ob mice.^[3] In vivo, linagliptin also exhibits time- and dose-dependent localization in kidney, liver, and intestine after intravenous dosing in rats.^[4]

Protocols

In vivo: Linagliptin is dissolved in physiological saline.^[4]

References

[1] 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 compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008, 325(1): 175-182. [2] Ishiguro N, et al. Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. Drug Metab Dispos. 2013, 41(1): 149-158. [3] Sch?rmann 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, 342(1): 71-80. [4] Greischel A, et al. The dipeptidyl peptidase-4 inhibitor linagliptin exhibits time- and dose-dependent localization in kidney, liver, and intestine after intravenous dosing: results from high resolution autoradiography in rats. Drug Metab Dispos. 2010, 38(9): 1443-1448.

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