What is the Linagliptin?

Linagliptin is , while it's Molecular Formula is C 25 H 28 N 8 O 2 . Labeled Linagliptin, intended for use as an internal standard for the quantification of Linagliptin by GC- or LC-mass spectrometry.

What is the CAS number for Linagliptin?

The CAS number of Linagliptin is 668270-12-0.

What is Linagliptin (668270-12-0) used for?

Linagliptin (trade names Tradjenta and Trajetna) is an inhibitor ofdipeptidyl peptidase-4 (DPP-4) that was approved by the U.S. FDA in May2011 for the treatment of Type 2 diabetes along with diet and exercise. Linagliptin (BI-1356) has beendescribed as a potent highly selective, slow-off rate and long acting inhibitor of DPP-4. Linagliptin arose from optimization efforts of xanthine-basedDPP-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 gavemuch reduced M1 affinity with no measureable hERG activity. Linagliptininhibits 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 upto 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-quinazolinegroup. Displacement of the bromide with (R)-Boc-3-amino-piperidinefollowed by deprotection gives linagliptin. When administered to db/dbmice orally, linagliptin dose dependently reduced glucose excursion from0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition).InChI:InChI=1/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

Product Class

668270-12-0

Product Name：Linagliptin
Molecular Formula：C₂₅H₂₈N₈O₂
Purity：99%
Molecular Weight：472.55

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Product Details:

CasNo： 668270-12-0

Molecular Formula： C₂₅H₂₈N₈O₂

Quality Factory Supply 668270-12-0 with Cheapest Price, Sale Linagliptin

Molecular Formula:C₂₅H₂₈N₈O₂
Molecular Weight:472.55
Vapor Pressure:0mmHg at 25°C
Melting Point:202 °C
Refractive Index:1.717
Boiling Point:661.189 °C at 760 mmHg
PKA:10.01±0.20(Predicted)
Flash Point:353.675 °C
PSA：116.86000
Density:1.398 g/cm³
LogP:1.91270

Linagliptin 668270-12-0 Factory

Linagliptin is in a class of medications called dipeptidyl peptidase-4 (DPP-4) inhibitors. It works by increasing the amounts of certain natural substances that lower blood sugar when it is high. Linagliptin is used together with proper diet and exercise to treat high blood sugar levels caused by type 2 diabetes mellitus. Hangzhou Huarong Pharm Co., Ltd. established since 2009 , has been always focusing on supplying products and services to our clients in the field of small molecule drug. At present, Huarong Pharm has successfully delivered innovative R&D products and services to more than 3,000 partners across the world. Our goal is to become a world-class leading company to support life science innovation and manufacturing.

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References

Clinical pharmacokinetics and pharmacodynamics of linagliptin

U Graefe-Mody, S Retlich, C Friedrich - Clinical pharmacokinetics, 2012

Review of linagliptin for the treatment of type 2 diabetes mellitus

JJ Neumiller, SM Setter - Clinical therapeutics, 2012

Linagliptin: a thorough characterization beyond its clinical efficacy

MA Sortino, T Sinagra, PL Canonico - Frontiers in endocrinology, 2013

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Product Class

668270-12-0

Product Details:

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Linagliptin 668270-12-0 Factory

References

Clinical pharmacokinetics and pharmacodynamics of linagliptin

Review of linagliptin for the treatment of type 2 diabetes mellitus

Linagliptin: a thorough characterization beyond its clinical efficacy

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