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Linagliptin

Cat. No. M2814
Linagliptin Structure
Synonym:

BI-1356

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 40  USD40 In stock
50mg USD 40  USD40 In stock
100mg USD 50  USD50 In stock
500mg USD 80  USD80 In stock
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Quality Control & Documentation
Biological Activity

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

Chemical Information
Molecular Weight 472.54
Formula C25H28N8O2
CAS Number 668270-12-0
Solubility (25°C) DMSO 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mark A Espeland, et al. Cardiovascular outcomes and safety with linagliptin, a dipeptidyl peptidase-4 inhibitor, compared with the sulphonylurea glimepiride in older people with type 2 diabetes: A subgroup analysis of the randomized CAROLINA trial

[2] Ildiko Lingvay, et al. Triple fixed-dose combination empagliflozin, linagliptin, and metformin for patients with type 2 diabetes

[3] Anton I Korbut, et al. SGLT2 Inhibitor Empagliflozin and DPP4 Inhibitor Linagliptin Reactivate Glomerular Autophagy in db/db Mice, a Model of Type 2 Diabetes

[4] Julio Rosenstock, et al. Effect of Linagliptin vs Placebo on Major Cardiovascular Events in Adults With Type 2 Diabetes and High Cardiovascular and Renal Risk: The CARMELINA Randomized Clinical Trial

[5] Khosro Keshavarz, et al. Linagliptin versus sitagliptin in patients with type 2 diabetes mellitus: a network meta-analysis of randomized clinical trials

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Keywords: Linagliptin, BI-1356 supplier, DPP, inhibitors, activators


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