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
