[CAS NO. 850649-61-5] Alogliptin

Name: Alogliptin
Brand: Arctom Scientific
SKU: SLK-S5365

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PRODUCTS SPECIFICATIONS [850649-61-5]

Store

Catalog

SLK-S5365

Brand

Selleck

CAS

850649-61-5

DESCRIPTION [850649-61-5]

Overview

MDL	MFCD09833196
Molecular Weight	339.39
Molecular Formula	C18H21N5O2
SMILES	C(N1C(=CC(=O)N(C)C1=O)N2C[C@H](N)CCC2)C3=C(C#N)C=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.9465 mL	14.7323 mL	29.4646 mL
5 mM	0.5893 mL	2.9465 mL	5.8929 mL
10 mM	0.2946 mL	1.4732 mL	2.9465 mL
50 mM	0.0589 mL	0.2946 mL	0.5893 mL

Description

Alogliptin is a potent, selective inhibitor of the with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.

Targets

DPP-4 ^[1]
(293E cells lysates)

2.93 nM

In vitro

Alogliptin is a potent (IC50 < 10 nM) inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM.

In vivo

Absolute oral bioavailability of alogliptin in rats, dogs, and monkeys is 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition is observed within 15 min and maximum inhibition is > 90% in rats, dogs, and monkeys; inhibition is sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). From Emax modeling, 50% inhibition of DPP-4 activity is observed at a mean alogliptin plasma concentration (EC50) of 3.4 to 5.6 ng/ml (10.0 to 16.5 nM) in rats, dogs, and monkeys. In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibites plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increases plasma GLP-1 (2- to 3-fold increase in AUC0–20 min) and increases early-phase insulin secretion (1.5- to 2.6-fold increase in AUC0-20 min) and reduces blood glucose excursion (31%–67% decrease in AUC0–90 min) after oral glucose challenge. Alogliptin (30 and 100 mg/kg) has no effect on fasting plasma glucose in normoglycemic rats..

References

[1] Huan Y, et al.J Pharmacol Toxicol Methods. 2015;71:8-12.
[2] Feng J, et al.J Med Chem. 2007,17;50(10):2297-300.
[3] Lee B, et al.Eur J Pharmacol. 2008,28;589(1-3):306-14.
[4] Moritoh Y, et al. Eur J Pharmacol. 2008,7;588(2-3):325-32.

Synonyms

Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-

2-[[6-[(3R)-3-Amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile

Alogliptin

(R)-2-[6-[3-Aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]benzonitrile

2-[[6-[(3R)-3-Aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile

Vipidia