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Merck
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SML3619

Sigma-Aldrich

Linagliptin

≥98% (HPLC)

Sinónimos:

(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, 8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione, BI 1356, BI-1356, BI1356, Ondero

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About This Item

Fórmula empírica (notación de Hill):
C25H28N8O2
Número de CAS:
668270-12-0
Peso molecular:
472.54
MDL number:
MFCD14635356
UNSPSC Code:
51111800
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Biochem/physiol Actions

Linagliptin is an orally active, competitive, potent and selective dipeptidyl peptidase IV (DPP4; DPP-IV) inhibitor (IC50 = 1 nM vs. 19 nM/sitagliptin, 24 nM/alogliptin, 50 nM/saxagliptin, 62 nM/vildagliptin) with no inhibitory potency against DPP-2/8/9 (IC50 >10 µM). Sitagliptin improves glucose tolerance and exhibits efficacy in diabetic rodent models in vivo (1-10 mg/kg via daily p.o. in mice and rats).

hcodes

H412

Hazard Classifications

Aquatic Chronic 3

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Matthias Eckhardt et al.
Journal of medicinal chemistry, 50(26), 6450-6453 (2007-12-07)
A new chemical class of potent DPP-4 inhibitors structurally derived from the xanthine scaffold for the treatment of type 2 diabetes has been discovered and evaluated. Systematic structural variations have led to 1 (BI 1356), a highly potent, selective, long-acting
Leo Thomas et al.
The Journal of pharmacology and experimental therapeutics, 325(1), 175-182 (2008-01-29)
BI 1356 [proposed trade name ONDERO; (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] is a novel dipeptidyl peptidase (DPP)-4 inhibitor under clinical development for the treatment of type 2 diabetes. In this study, we investigated the potency, selectivity, mechanism, and duration of action of BI 1356
Leo Thomas et al.
The Journal of pharmacology and experimental therapeutics, 328(2), 556-563 (2008-10-31)
Antidiabetic effects of dipeptidyl peptidase-4 (DPP-4) inhibitors are exerted by potentiation of the biological activity of incretin hormones like glucagon-like peptide (GLP)-1. BI 1356 [proposed trade name Ondero; (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] is a novel competitive, selective, potent, and long-acting DPP-4 inhibitor under

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