[CAS NO. 850649-62-6] AlogliptinBenzoate

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PRODUCTS SPECIFICATIONS [850649-62-6]

Catalog

HY-A0023

Brand

MCE

CAS

850649-62-6

DESCRIPTION [850649-62-6]

Overview

MDL	MFCD09833195
Molecular Weight	461.51
Molecular Formula	C25H27N5O4
SMILES	O=C(C=C(N1C[C@H](N)CCC1)N(C2=O)CC3=C(C#N)C=CC=C3)N2C.O=C(O)C4=CC=CC=C4

For research use only. We do not sell to patients.

5 Publications Citing Use of MCE

Summary

Alogliptin Benzoate (SYR-322) is a potent, selective and orally active inhibitor of DPP-4 with an IC ₅₀ of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin Benzoate can be used for the research of type 2 diabetes ^[1] ^[2] ^[3] .

IC50 & Target

IC50: <10 nM (DPP-4) ^[1]

In Vitro

Alogliptin (1 nM; 5-60 min) inhibits LPS-induced extracellular signal-regulated kinase (ERK) phosphorylation in U937 cells ^[2] .
Alogliptin (0.5-5 nM; 24 h) inhibits LPS-stimulated MMP-1 secretion and mRNA expression that is mediated by ERK pathway in U937 cells ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Alogliptin (0.01-1 mg/kg; p.o.) produced dose-dependent improvements in glucose tolerance and increased plasma insulin levels in female Wistar fatty rats ^[1] .
Alogliptin (40 mg/kg/day for 2 weeks; p.o.) reduces infarction area and improves brain vascular integrity in middle cerebral artery occlusion (MCAO) mice ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05363592	Celltrion	Type 2 Diabetes	June 25, 2022	Phase 1
NCT00707993	Takeda	Diabetes Mellitus	June 2008	Phase 3
NCT00968708	Takeda	Diabetes Mellitus, Type 2\|Acute Coronary Syndrome	September 2009	Phase 3
NCT00763347	Takeda	Diabetes Mellitus	November 2006	Phase 2
NCT03555565	Takeda	Type 2 Diabetes Mellitus	February 28, 2017
NCT01632007	Takeda	Diabetes Mellitus	May 2012	Phase 3
NCT03501277	Takeda	Healthy Volunteers	May 26, 2018	Phase 1
NCT00957268	Takeda	Diabetes Mellitus, Type 2	September 2009	Phase 1
NCT00286494	Takeda	Diabetes Mellitus	February 2006	Phase 3
NCT01664624	AstraZeneca	Type 2 Diabetes	July 2012	Phase 1
NCT00328627	Takeda	Type 2 Diabetes Mellitus	May 2006	Phase 3
NCT02756832	Takeda	Diabetes Mellitus	September 20, 2016
NCT01890122	Takeda	Diabetes Mellitus	September 2013	Phase 3
NCT00655863	Takeda	Diabetes Mellitus	July 2007	Phase 3
NCT02221284	Takeda	Type 2 Diabetes Mellitus	June 30, 2014
NCT01023581	Takeda	Diabetes Mellitus, Type 2	November 2009	Phase 3
NCT02508168	Takeda	Healthy Volunteers	April 2016	Phase 1
NCT00286429	Takeda	Diabetes Mellitus	February 2006	Phase 3
NCT02798172	Fourth People´s Hospital of Shenyang	Diabetes Mellitus, Type 2	May 2014	Not Applicable
NCT03042325	Takeda	Diabetes Mellitus, Type 2	July 30, 2017	Phase 4
NCT01964963	Takeda	Type 2 Diabetes Mellitus	August 3, 2011
NCT00286468	Takeda	Diabetes Mellitus	April 2006	Phase 3
NCT01263496	Takeda	Type 2 Diabetes Mellitus	May 2007	Phase 2
NCT04470310	Seoul National University Hospital	Type 2 Diabetes Mellitus	December 31, 2015	Phase 4
NCT01318109	Takeda	Type 2 Diabetes Mellitus	August 2008	Phase 2\|Phase 3
NCT01456130	Takeda	Diabetes Mellitus	November 2011	Phase 3
NCT01318122	Takeda	Type 2 Diabetes Mellitus	May 2008	Phase 2\|Phase 3
NCT00755846	Takeda	Diabetes Mellitus	March 2005	Phase 2
NCT03231709	Takeda	Type 2 Diabetes Mellitus	August 18, 2017	Phase 4
NCT04392557	University of Catanzaro	Diabetes Mellitus, Type 2	July 1, 2020	Phase 4
NCT00286455	Takeda	Diabetes Mellitus	February 2006	Phase 3
NCT01945242	Takeda	Type 2 Diabetes Melitus	March 2011
NCT02231021	Kun-Ho Yoon\|Takeda\|The Catholic University of Korea	Type 2 Diabetes Mellitus	September 2014	Phase 4
NCT01945216	Takeda	Type 2 Diabetes Mellitus Who Have Been Examined at a Medical Institution	July 8, 2010
NCT02856113	Takeda\|Takeda Development Center Americas, Inc.	Diabetes Mellitus, Type 2	October 14, 2016	Phase 3
NCT01303055	Aichi Gakuin University	Diabetes Mellitus, Type 2	February 2011	Not Applicable
NCT00432276	Takeda	Diabetes Mellitus	January 2007	Phase 3
NCT02771093	Takeda	Type 2 Diabetes Mellitus	September 8, 2016	Phase 4
NCT01318070	Takeda	Type 2 Diabetes Mellitus	November 2007	Phase 2\|Phase 3
NCT02068443	Takeda	Type 2 Diabetes Mellitus	February 2014	Phase 3
NCT01263483	Takeda	Type 2 Diabetes Mellitus	January 2007	Phase 2\|Phase 3
NCT00856284	Takeda	Type 2 Diabetes Mellitus	March 2009	Phase 3
NCT00306384	Takeda	Diabetes Mellitus	March 2006	Phase 3
NCT02989649	Takeda	Diabetes Mellitus, Type 2	December 22, 2016
NCT00286442	Takeda	Diabetes Mellitus	March 2006	Phase 3
NCT01263470	Takeda	Diabetes Mellitus, Type 2	January 2007	Phase 2
NCT02763007	Kun-Ho Yoon\|Takeda\|The Catholic University of Korea	Diabetes Mellitus, Type 2	May 18, 2016	Phase 4
NCT05363384	Celltrion	Type 2 Diabetes	June 11, 2022	Phase 1
NCT01318135	Takeda	Type 2 Diabetes Mellitus	January 2009	Phase 2\|Phase 3
NCT01391663	Takeda	Pharmacokinetics and Pharmacodynamics	July 2011	Phase 1
NCT04980040	Takeda	Type 2 Diabetes Mellitus	April 19, 2014
NCT01289119	Takeda	Diabetes Mellitus, Type 2	December 2010	Phase 3
NCT01318083	Takeda	Type 2 Diabetes Mellitus	August 2008	Phase 2\|Phase 3
NCT03794336	Sanofi	Type 2 Diabetes Mellitus	June 29, 2019	Phase 4
NCT00395512	Takeda	Diabetes Mellitus	November 2006	Phase 3
NCT01588587	Nagaoka Red Cross Hospital\|Kurume University	Type 2 Diabetes Mellitus	October 2012
NCT03499704	Celltrion Pharm, Inc.	Diabetes Mellitus, Type 2	February 11, 2020	Phase 4
NCT01521962	Takeda	Diabetes Mellitus	February 2012	Phase 3
NCT01263509	Takeda	Type 2 Diabetes Mellitus	June 2007	Phase 2\|Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 54.17 mM ; ultrasonic and warming and heat to 60°C)

H ₂ O : 14.29 mg/mL ( 30.96 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1668 mL	10.8340 mL	21.6680 mL
5 mM	0.4334 mL	2.1668 mL	4.3336 mL
10 mM	0.2167 mL	1.0834 mL	2.1668 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.25 mg/mL (2.71 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.25 mg/mL (2.71 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.25 mg/mL (2.71 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

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

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

SYR 322

Alogliptin benzoate

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