Reagents and instruments for immunology, cell biology and molecular biology.

Alogliptin [850649-61-5]

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Cat# HY-A0023A-5mg

Size : 5mg

Brand : MedChemExpress

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Description

Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC₅₀ of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes^[1]^[2]^[3].

IC₅₀ & Target

DPP-4

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	24 nM Compound: Alogliptin	Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay	[PMID: 23623674]
Sf9	IC₅₀	> 100 μM Compound: Alogliptin	Inhibition of recombinant full-length human N-terminal GST-tagged DPP8 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay Inhibition of recombinant full-length human N-terminal GST-tagged DPP8 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay	[PMID: 30642693]
Sf9	IC₅₀	> 100 μM Compound: Alogliptin	Inhibition of recombinant full-length human N-terminal GST-tagged DPP9 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay Inhibition of recombinant full-length human N-terminal GST-tagged DPP9 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay	[PMID: 30642693]
Sf9	IC₅₀	2.7 nM Compound: Alogliptin	Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay	[PMID: 30642693]
Sf9	IC₅₀	4.46 nM Compound: Alogliptin	Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition measured at 60 secs interval for 20 mins by fluorometic method Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition measured at 60 secs interval for 20 mins by fluorometic method	[PMID: 31336309]
U-87MG ATCC	IC₅₀	1470 μM Compound: Alogliptin	Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay	[PMID: 32527554]

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].

MedChemExpress (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].

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

Clinical Trial

Molecular Weight

339.40

Formula

C₁₈H₂₁N₅O₂

CAS No.

850649-61-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(C=C(N1C[C@H](N)CCC1)N(C2=O)CC3=C(C#N)C=CC=C3)N2C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (294.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 10 mg/mL (29.46 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9464 mL	14.7319 mL	29.4638 mL
5 mM	0.5893 mL	2.9464 mL	5.8928 mL
10 mM	0.2946 mL	1.4732 mL	2.9464 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.76%

Data Sheet (278 KB) SDS (597 KB)

COA (252 KB) HNMR (273 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Feng J, et al. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J Med Chem. 2007 May 17;50(10):2297-300. [Content Brief]

[2]. Ta NN, et al. DPP-4 (CD26) inhibitor alogliptin inhibits TLR4-mediated ERK activation and ERK-dependent MMP-1 expression by U937 histiocytes. Atherosclerosis. 2010 Dec;213(2):429-35. [Content Brief]

[3]. Hao FL, et, al. The neurovascular protective effect of alogliptin in murine MCAO model and brain endothelial cells. Biomed Pharmacother. 2019 Jan;109:181-187. [Content Brief]

[4]. Asakawa T, et al. A novel dipeptidyl peptidase-4 inhibitor, alogliptin (SYR-322), is effective in diabetic rats with sulfonylurea-induced secondary failure. Life Sci. 2009 Jul 17;85(3-4):122-6. [Content Brief]

[5]. Moritoh Y, et al. The dipeptidyl peptidase-4 inhibitor alogliptin in combination with pioglitazone improves glycemic control, lipid profiles, and increases pancreatic insulin content in ob/ob mice. Eur J Pharmacol. 2009 Jan 14;602(2-3):448-54. [Content Brief]

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Alogliptin [850649-61-5]

Cat# HY-A0023A-5mg

Brand : MedChemExpress

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