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Linagliptin

CAS:
668270-12-0
MF:
C25H28N8O2
MW:
472.54

Properties

Melting point:
202 ºC
Boiling point:
661.2±65.0 °C(Predicted)
Density 
1.39
pka
10.01±0.20(Predicted)

Safety Information

HS Code 
29335990

Use

Linagliptin (trade names Tradjenta and Trajetna) is an inhibitor of dipeptidyl peptidase-4 (DPP-4) that was approved by the U.S. FDA in May 2011 for the treatment of Type 2 diabetes along with diet and exercise. Linagliptin (BI-1356) has been described as a potent highly selective, slow-off rate and long acting inhibitor of DPP-4. Linagliptin arose from optimization efforts of xanthine-based DPP-4 inhibitors with the initial lead identified from an HTS campaign. After optimizing the activity of the initial micromolar lead, two issues that needed to be addressed were activity for hERG and muscarinic receptor M1. Introduction of a butynyl group at the N7 position of the xanthine ring gave much reduced M1 affinity with no measureable hERG activity. Linagliptin inhibits DPP-4 with an IC50=1 nM and is highly selective (>10,000-fold) against DPP-8 and DPP-9. Linagliptin shows no interactions with CYPs up to 50 mM. The described synthesis of linagliptin starts with 8-bromoxanthine, which is alkylated at the N-7 position to introduce the butyne group, followed by alkylation of the N-1 group to introduce the methyl-quinazoline group. Displacement of the bromide with (R)-Boc-3-amino-piperidine followed by deprotection gives linagliptin. When administered to db/db mice orally, linagliptin dose dependently reduced glucose excursion from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition).

357 supplier list of "Linagliptin"

  • Product Name:Linagliptin
  • Products Intro:Purity: 0.99 | Package: 1kg 25kg 200 kilograms per barrel
  • Company Type: Trader
  • Country/Region: CHINA
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  • Products Intro:Purity: 99% | Package: As customer's requirement
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  • Country/Region: CHINA
  • Product Name:Linagliptin
  • Products Intro:Purity: 99%+ | Package: 1g;USD|10g;USD|100g;USD|1KG;USD
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  • Country/Region: CHINA

    $1.00/ 1KG

  • Product Name:Linagliptin
  • Products Intro:Purity: 98%|Package: 1KG;1USD
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  • Country/Region: CHINA
  • Main Products: Tianeptine Sulphate

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  • Products Intro:Purity: 99%|Package: 25KG;0USD
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  • Country/Region: CHINA
  • Main Products: Molnupiravir

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  • Products Intro:Purity: 99.99%|Package: 1KG;20USD
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  • Country/Region: CHINA
  • Main Products: 22563-90-2

    $0.01-1 / 1KG

  • Product Name:Linagliptin
  • Products Intro:Purity: 99%+|Package: 1KG;0.01USD|25KG;0.1USD|100KG;1USD
  • Company Type: Trader
  • Country/Region: CHINA
  • Product Name:Linagliptin
  • Company Type: Service provider
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  • Product Name:Linagliptin
  • Products Intro:Purity: 99.0% | Package: 1KG;USD
  • Company Type: Reagent
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  • Main Products: Speciality Chemicals
  • Product Name:Linagliptin
  • Products Intro:Purity: 98% | Package: 100G;1KG;5KG;10KG;25KG;50KG;100KG
  • Company Type: Trader
  • Country/Region: CHINA

Linagliptin Related Search:

Ruxolitinib phosphateLinagliptin Impurity B8-bromo-7-(but-2-ynyl)-3-methyl-1H-purine-2,6(3H,7H)-dioneLinagliptin Impurity 4Linagliptin Impurity ILinagliptin iMpurity GLinagliptin Impurity DLinagliptin Impurity 5Linagliptin Impurity K8-Bromo-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dioneLinagliptin iMpurity ELIMAPROSTlifitegrast2-ButyneDROPERIDOLMethyl celluloseHaloperidolQuinazoline
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