Linagliptin

For research use only. Not for therapeutic Use.

  • CAT Number: A000890
  • CAS Number: 668270-12-0
  • Molecular Formula: C₂₅H₂₆N₈O₂
  • Molecular Weight: 472.54
  • Purity: ≥95%
Inquiry Now

Linagliptin(Cat No.:A000890)is a dipeptidyl peptidase-4 (DPP-4) inhibitor used in the management of type 2 diabetes, aimed at improving glycemic control. By inhibiting DPP-4, linagliptin prolongs the activity of incretin hormones, enhancing insulin secretion and suppressing glucagon release in response to meals. This action helps regulate blood glucose levels without significant risk of hypoglycemia. Unique among DPP-4 inhibitors, linagliptin is minimally excreted through the kidneys, making it suitable for patients with renal impairment. It is widely studied for its efficacy, safety, and potential cardiometabolic benefits in diabetes care.


Catalog Number A000890
CAS Number 668270-12-0
Synonyms

668270-12-0; Tradjenta; Ondero; BI-1356; BI 1356

Molecular Formula C₂₅H₂₆N₈O₂
Purity ≥95%
Target DPP-4
Solubility >17.9mg/mL in DMSO
Storage -20°C
IUPAC Name 8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
InChI InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1
InChIKey LTXREWYXXSTFRX-QGZVFWFLSA-N
SMILES CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
Reference

1: Li YR, Tsai SS, Chen DY, Chen ST, Sun JH, Chang HY, Liou MJ, Chen TH.
Linagliptin and cardiovascular outcomes in type 2 diabetes after acute coronary
syndrome or acute ischemic stroke. Cardiovasc Diabetol. 2018 Jan 4;17(1):2. doi:
10.1186/s12933-017-0655-y. PubMed PMID: 29301579; PubMed Central PMCID:
PMC5753457.
<br>

2: Umpierrez GE, Cardona S, Chachkhiani D, Fayfman M, Saiyed S, Wang H, Vellanki
P, Haw JS, Olson DE, Pasquel FJ, Johnson TM 2nd. A Randomized Controlled Study
Comparing a DPP4 Inhibitor (Linagliptin) and Basal Insulin (Glargine) in Patients
With Type 2 Diabetes in Long-Term Care and Skilled Nursing Facilities:
Linagliptin-LTC Trial. J Am Med Dir Assoc. 2017 Dec 27. pii:
S1525-8610(17)30629-1. doi: 10.1016/j.jamda.2017.11.002. [Epub ahead of print]
PubMed PMID: 29289540.
<br>

3: Zhang Y, Fava GE, Wu M, Htun W, Klein T, Fonseca VA, Wu H. Effects of
Linagliptin on Pancreatic α Cells of Type 1 Diabetic Mice. J Endocr Soc. 2017 Aug
31;1(10):1224-1234. doi: 10.1210/js.2017-00253. eCollection 2017 Oct 1. PubMed
PMID: 29264448; PubMed Central PMCID: PMC5686619.
<br>

4: Rizos CV, Filippatos TD, Elisaf MS. Pharmacokinetic drug evaluation of
empagliflozin plus linagliptin for the treatment of type 2 diabetes. Expert Opin
Drug Metab Toxicol. 2018 Jan;14(1):117-125. doi: 10.1080/17425255.2018.1418325.
Epub 2017 Dec 19. Review. PubMed PMID: 29241374.
<br>

5: Bahirat UA, Shenoy RR, Talwar R, Goel RN, Nemmani KVS. Co-administration of
APD668, a G protein-coupled receptor 119 agonist and linagliptin, a DPPIV
inhibitor, prevents progression of steatohepatitis in mice fed on a high
trans-fat diet. Biochem Biophys Res Commun. 2018 Jan 8;495(2):1608-1613. doi:
10.1016/j.bbrc.2017.12.004. Epub 2017 Dec 5. PubMed PMID: 29203247.
<br>

6: Hasegawa Y, Hayashi K, Takemoto Y, Cheng C, Takane K, Lin B, Komohara Y,
Kim-Mitsuyama S. DPP-4 inhibition with linagliptin ameliorates the progression of
premature aging in klotho-/- mice. Cardiovasc Diabetol. 2017 Dec 1;16(1):154.
doi: 10.1186/s12933-017-0639-y. PubMed PMID: 29195509; PubMed Central PMCID:
PMC5709858.
<br>

7: Tamborlane WV, Laffel LM, Weill J, Gordat M, Neubacher D, Retlich S, Hettema
W, Hoesl CE, Kaspers S, Marquard J. Randomized, double-blind, placebo-controlled
dose-finding study of the dipeptidyl peptidase-4 inhibitor linagliptin in
pediatric patients with type 2 diabetes. Pediatr Diabetes. 2017 Nov 24. doi:
10.1111/pedi.12616. [Epub ahead of print] PubMed PMID: 29171139.

<br>
8: Catic T, Lekic L, Zah V, Tabakovic V. Budget Impact of Introducing Linagliptin
into Bosnia and Herzegovina Health Insurance Drug Reimbursement List in
2016-2018. Mater Sociomed. 2017 Sep;29(3):176-181. doi:
10.5455/msm.2017.29.176-181. PubMed PMID: 29109662; PubMed Central PMCID:
PMC5644199.
<br>

9: Keshavarz K, Lotfi F, Sanati E, Salesi M, Hashemi-Meshkini A, Jafari M,
Mojahedian MM, Najafi B, Nikfar S. Linagliptin versus sitagliptin in patients
with type 2 diabetes mellitus: a network meta-analysis of randomized clinical
trials. Daru. 2017 Oct 25;25(1):23. doi: 10.1186/s40199-017-0189-6. Review.
PubMed PMID: 29070077; PubMed Central PMCID: PMC5655990.
<br>

10: Satoh H, Ohira T, Moriya C, Inoue I, Kuribayashi S, Seino H, Hirai H, Hiyoshi
T, Watada H; L-CGM Study Group. Effects of linagliptin vs. voglibose on daily
glucose excursions during continuous glucose monitoring of Japanese type 2
diabetes patients (L-CGM): A randomized, open-label, two-arm, parallel
comparative trial. Diabetes Metab. 2017 Dec;43(6):550-553. doi:
10.1016/j.diabet.2017.07.010. Epub 2017 Sep 22. PubMed PMID: 28947255.

Request a Quote