Linagliptin
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MedKoo CAT#: 300125

CAS#: 668270-12-0

Description: Linagliptin, also known as BI-1356, is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes. Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly.


Chemical Structure

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Linagliptin
CAS# 668270-12-0

Theoretical Analysis

MedKoo Cat#: 300125
Name: Linagliptin
CAS#: 668270-12-0
Chemical Formula: C25H28N8O2
Exact Mass: 472.23352
Molecular Weight: 472.54
Elemental Analysis: C, 63.54; H, 5.97; N, 23.71; O, 6.77

Price and Availability

Size Price Availability Quantity
100.0mg USD 60.0 Same day
200.0mg USD 70.0 Same day
500.0mg USD 90.0 Same day
1.0g USD 150.0 Same day
2.0g USD 250.0 Same day
5.0g USD 450.0 Same day
10.0g USD 850.0 Same day
20.0g USD 1250.0 Same day
50.0g USD 2150.0 Same day
100.0g USD 2850.0 Same day
200.0g USD 3950.0 Same day
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Synonym: BI1356; BI 1356; BI-1356; Linagliptin. trade names Tradjenta and Trajenta

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

InChi Key: LTXREWYXXSTFRX-QGZVFWFLSA-N

InChi Code: 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

SMILES Code: O=C(N1CC2=NC(C)=C3C=CC=CC3=N2)N(C)C4=C(N(CC#CC)C(N5C[C@H](N)CCC5)=N4)C1=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO.

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 472.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Linagliptin. Avoid gliptins! Prescrire Int. 2013 Feb;22(135):36-7. Review. PubMed PMID: 23444496.

2: Brown DX, Choudhury M, Evans M. Linagliptin as add-on therapy for type 2 diabetes - an overview. Drugs Today (Barc). 2012 Oct;48(10):645-54. doi: 10.1358/dot.2012.48.10.1860771. Review. PubMed PMID: 23110260.

3: Deeks ED. Linagliptin: a review of its use in the management of type 2 diabetes mellitus. Drugs. 2012 Sep 10;72(13):1793-824. doi: 10.2165/11209570-000000000-00000. Review. Erratum in: Drugs. 2013 Jan;73(1):99. PubMed PMID: 22913735.

4: Graefe-Mody U, Retlich S, Friedrich C. Clinical pharmacokinetics and pharmacodynamics of linagliptin. Clin Pharmacokinet. 2012 Jul 1;51(7):411-27. doi: 10.2165/11630900-000000000-00000. Review. PubMed PMID: 22568694.

5: Ohmura T, Hayashi N, Encinas J. [Pharmacological and clinical profiles of the DPP-4 inhibitor linagliptin (Trazenta)]. Nihon Yakurigaku Zasshi. 2012 Apr;139(4):174-83. Review. Japanese. PubMed PMID: 22498683.

6: Neumiller JJ, Setter SM. Review of linagliptin for the treatment of type 2 diabetes mellitus. Clin Ther. 2012 May;34(5):993-1005. doi: 10.1016/j.clinthera.2012.02.029. Epub 2012 Mar 21. Review. PubMed PMID: 22440191.

7: Agrawal R, Jain P, Dikshit SN. Linagliptin: a novel methylxanthin based approved dipeptidyl peptidase-4 inhibitor. Curr Drug Targets. 2012 Jun;13(7):970-83. Review. PubMed PMID: 22420306.

8: Singh-Franco D, McLaughlin-Middlekauff J, Elrod S, Harrington C. The effect of linagliptin on glycaemic control and tolerability in patients with type 2 diabetes mellitus: a systematic review and meta-analysis. Diabetes Obes Metab. 2012 Aug;14(8):694-708. doi: 10.1111/j.1463-1326.2012.01586.x. Epub 2012 Mar 20. Review. PubMed PMID: 22340363.

9: Neumiller JJ. Pharmacology, efficacy, and safety of linagliptin for the treatment of type 2 diabetes mellitus. Ann Pharmacother. 2012 Mar;46(3):358-67. doi: 10.1345/aph.1Q522. Epub 2012 Feb 7. Review. PubMed PMID: 22318932.

10: Forst T, Pfützner A. Linagliptin, a dipeptidyl peptidase-4 inhibitor with a unique pharmacological profile, and efficacy in a broad range of patients with type 2 diabetes. Expert Opin Pharmacother. 2012 Jan;13(1):101-10. doi: 10.1517/14656566.2012.642863. Review. PubMed PMID: 22149370.