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Linagliptin

Linagliptin
Linagliptin structure
CAS No.
668270-12-0
Chemical Name:
Linagliptin
Synonyms
Ondero;Bi 1356;Tradjenta;Linaglitine;linagliptin;Linagliptin-D4;Linagliptin API;Linagliptin, >=98%;Linagliptin (BI-1356);Linagliptin (668270-12-0)
CBNumber:
CB71518518
Molecular Formula:
C25H28N8O2
Formula Weight:
472.54
MOL File:
668270-12-0.mol

Linagliptin Properties

Melting point:
202 ºC
Density 
1.39

SAFETY

Linagliptin price More Price(3)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 23306 Linagliptin ≥98% 668270-12-0 100mg $49 2018-11-19 Buy
Cayman Chemical 23306 Linagliptin ≥98% 668270-12-0 500mg $98 2018-11-19 Buy
Cayman Chemical 23306 Linagliptin ≥98% 668270-12-0 1g $184 2018-11-19 Buy

Linagliptin Chemical Properties,Uses,Production

Description

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).

Originator

Boehringer Ingelheim (United States)

Uses

A novel potent and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with potential use in the treatment of type 2 diabetes.

Uses

dipeptidypeptidase inhibitor, antidiabetic

Uses

highly potent CD26 inhibitor

Uses

Labeled Linagliptin, intended for use as an internal standard for the quantification of Linagliptin by GC- or LC-mass spectrometry.

Definition

ChEBI: A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type I diabetes.

brand name

Tradjenta

Linagliptin Preparation Products And Raw materials

Raw materials

Preparation Products


Linagliptin Suppliers

Global( 297)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 887 50
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3217 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22043 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Shanghai Time Chemicals CO., Ltd.
+86-021-57951555
+86-021-57951555 jack.li@time-chemicals.com CHINA 1374 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2548 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070;product@chemlin.com.cn
product@chemlin.com.cn CHINA 3015 60
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 663 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 16534 60

View Lastest Price from Linagliptin manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-07-25 Linagliptin
668270-12-0
US $100.00 / KG 100G 98% 200KG career henan chemical co
2018-07-19 Linagliptin (668270-12-0)
668270-12-0
US $100.00-10.00 / G 10UG 99% 1000kg/month Hebei Chisure Biotechnology Co., Ltd.

668270-12-0(Linagliptin)Related Search:


  • Tradjenta
  • Linagliptin-D4
  • Linagliptin (BI-1356)
  • Linaglitine
  • (R)-8-(3-aMinopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H-purine-2,6(3H,7H)-dione
  • Linagliptin API
  • 1H-Purine-2,6-dione,8-[(3R)-3-aMino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-
  • (R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione
  • Linagliptin 8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione
  • Linagliptin, >=98%
  • linagliptin / 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-
  • 8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-Met
  • Linagliptin (668270-12-0)
  • linagliptin
  • 8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione
  • -
  • Pharmaceutical raw material
  • Inhibitor
  • Linagliptin
  • TRADJENTA
  • Amines
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • API
  • (R)-8-(3-Amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione
  • 1H-Purine-2,6-dione, 8-((3R)-3-amino-1-piperidinyl)-7-(2-butynyl)-3,7-dihydro-3-methyl-1-((4-methyl-2-quinazolinyl)methyl)-
  • Bi 1356
  • Ondero
  • 8-[(3R)-3-aMinopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-Methyl-1-[(4-Methylquinazolin-2-yl)Methyl]-2,3,6,7-tetrahydro-1H-purine-2,6-dione
  • 8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-1H-purine-2,6-dione
  • 8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-1H-purine-2,6-d
  • 668270-12-0
  • C25H28N8O2
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