Linagliptin CAS: 668270-12-0
MF: C25H28N8O2
MW: 472.54

Linagliptin (CAS 668270-12-0)

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別名: Linagliptin is also known as BI-1356.
アプリケーション: Linagliptin is a highly potent CD26 (DPP-4) inhibitor with over 10,000-fold selectivity over other peptidases and proteases.
CAS 番号: 668270-12-0
Molecular Weight: 472.54
Molecular Formula: C25H28N8O2
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* Refer to Certificate of Analysis for lot specific data (including water content).
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Linagliptin is a highly potent, selective CD26 (DPP-4) inhibitor with IC50 of 1 nM. Linagliptin was observed to be 10,000-fold more selective for DPP-4 over 11 other peptidases and proteases studied in a test. Linagliptin can also inhibit up to 90% of DPP-4 activity in rat plasma. In Zucker diabetic fatty rats, Linagliptin can dose-dependently decrease plasma glucose and increase plasma levels of glucagon-like peptide 1 and insulin. When administered orally, Linagliptin reduced HbA1c levels in mice with high-fat diets and low-dose streptozotocin-induced diabetes. Type 2 diabetes mellitus has been treated using formulations containing Linagliptin.


参考文献

1. Thomas, L., Eckhardt, M., Langkopf, E., 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. 325(1), 175-182 (2008).
2. Thomas, L., tadayyon, M., and Mark, M.Chronic treatment with the dipeptidyl peptidase-4 inhibitor BI 1356 [(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] increases basal glucagon-like peptide-1 and improves glycemic control in diabetic rodent models. J. Pharmacol. Exp. Ther. 328(2), 556-563 (2009).
3. Ning, G., Bandgar, T., Hehnke, U., et al.Efficacy and safety of linagliptin in 2681 Asian patients stratified by age, obesity, and renal function: A pooled analysis of randomized clinical trials. Adv. Ther. (2017).

Physical State :
Solid
Solubility :
Soluble in DMSO (17 mg/ml at 25° C), water (<1 mg/ml at 25° C), ethanol (1 mg/ml at 25° C), 0.5% hyroxyethylcellulose (30 mg/ml at 25° C), and methanol.
保存方法 :
Store at -20° C
Melting Point :
190-196° C
Boiling Point :
~661.2° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.72 (Predicted)
IC50 :
CD26: IC50 = 0.1 nM (human); FAPα: IC50 = 89 nM (human); mAChR M1: IC50 = 295 nM (human); Seprase: IC50 = 370 nM (mouse); DPRP2: IC50 >10 µM (human)
pK Values :
pKb: 10.1 (Predicted)
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PubChem CID :
MDL Number :
MFCD14635356
SMILES :
CC#CCN1C2=C(N=C1N3CCC[[email protected]](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C

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