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Product Name: Linagliptin (BI-1356)

CAS No.: 668270-12-0

Information: DDP-4 inhibitor,highly potent and competitive

Description: Linagliptin is a highly potent, competitive inhibitor of dipeptidyl-peptidase 4 (DDP-4) with IC50 value of 1 nM.

Chemical Name: 8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione

Canonical SMILES: CC#CCN1C2=C(N=C1N3CCCC(C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C

MF: C25H28N8O2

MW: 472.54

Purity: GC>99.7%

Single purity:<0.2%

Appearance: Off-white powder

Type: Antidiabetic agents

Model Number: API-Linagliptin

Solubility: Soluble in DMSO > 10 mM 

Storage: Store at -20°C 

General tips: For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. 

Shipping Condition: Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request

Background: BI1356 is a potent and competitive DPP-4 inhibitor, which exhibited DPP-4 inhibiting activity in several independent tests with IC50 values of 0.4, 0.5, 0.9, and 1.1nM.[1]

DPP-4 is an N-terminal dipeptidyl exopeptidase existing as a membrane-bound protein and also as a soluble protein in plasma. It plays a major role in the degradation of incretins such as GLP-1 which is of great importance in the process of glucose metabolism. Under physiological conditions, GLP-1 is truncated by DPP-4 rapidly, which is located on the capillary endothelium proximal to the L-cells where GLP-1 is secreted in the ileum. GLP-1 could sensitize β-cells to glucose stimulation,consequently increasing intracellular cAMP concentrations in β-cells and accelerating and augmenting insulin response to absorb glucose. By being measured at the substrate at the binding site, BI1356 inhibits the DPP-4 enzyme.[1]

DPP-4 was extracted from confluent Caco-2 cells to determine the inhibition activity of BI1356. Assays were performed by mixing the inhibitor solution with substrates and the Caco-2 cell extract, which illustrated BI1356 inhibited DPP-4 with IC 50 values of 0.4, 0.5, 0.9, and 1.1 nM. BI1356 also possesses a very significant selectivity for DPP-4 relative to other dipeptidyl peptidases aminopeptidases N and P, prolyloligopeptidase, and the proteases trypsin, plasmin, and thrombin.[1]

An in vivo evaluation showed that BI1356 dose-dependently inhibited the DPP-4 enzyme in plasma within 30 min of administration. Separate doses ranging from 1 to 10 mg/kg achieved significant inhibition activity of DPP-4, which also showed persistent DPP-4 inhibition activity. The ED50 value for inhibition of plasma DPP-4 activity was calculated to be 0.9 mg/kg 24 h post dose. In a clinical study,  BI1356 produced a remarkable, clinically meaningful and persistent improvement in glycaemic control, in accordance with enhanced parameters of β-cell function.  Patients treated with BI1356 were more likely to achieve a reduction in HbA1c of ≥ 0.5% comparing control.[1,2]

Brand Name: Huavet

Place of Origin: Shaanxi,China (Mainland)

USAGE: Pharmaceutical Intermediates

COA: Available

MSDS: Available

Spectrum: Available

Inventory status: in stock

Assay: 99% min

Shelf life: 2 years

Packaging Details: 1g,5g,10g,50g,100g/bottle, 1kg/tin for trial order,25kg/drum for commercial quantity. Specific packing required by customer

for Lesinurad.

Delivery Detail: Prompt shipment