Alogliptin
Based on 6 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 850649-61-5
- Formel: C18H21N5O2
- Molecular Weight:339.40
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Metabolism/Protease Compound Library
HY-L012
-
FDA-Approved Drug Library
HY-L022
-
Drug Repurposing Compound Library
HY-L035
-
Anti-diabetic Compound Library
HY-L040
-
Ferroptosis Compound Library
HY-L051
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
EMA-Approved Drug Library
HY-L116
-
Human Metabolite Library
HY-L123
-
Heterocyclic Compound Library
HY-L138
-
Off-patent Drug Library
HY-L141
-
Metabolic Enzyme Compound Library
HY-L146
-
Protease Inhibitor Library
HY-L147
-
Highly Selective Inhibitors Library
HY-L158
-
Cell Death Library
HY-L162
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Amino Acid Metabolism Compound Library
HY-L189
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
MCE Kinase Hinge Binder Fragment Library
HY-L907
Publications Citing Use of MedChemExpress (MCE) Alogliptin
More
Customer Validation & Images
-
WB
Biologische Aktivität
|
DPP-4 |
|
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] |
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.
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.
Chemical Information
-
CAS. Nr. 850649-61-5
-
Appearance Solid
-
Molecular Weight 339.40
-
Formel C18H21N5O2
-
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
-
Synonyms
SYR-322 free base
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
-
Journal Impact Factor
-
Most Recent
-
Sci Signal
Tyrosine kinase inhibitors can activate the NLRP3 inflammasome in myeloid cells through lysosomal damage and cell lysis. [Abstract]2023 Jan 17;16(768):eabh1083. PMID: 36649377 -
Sci Rep
2019 Dec 2;9(1):18094. PMID: 31792328 -
Biol Chem
The Mycobacterium tuberculosis prolyl dipeptidyl peptidase cleaves the N-terminal peptide of the immunoprotein CXCL-10. [Abstract]2023 Jan 12;404(6):633-643. PMID: 36632703 -
Biochem Biophys Res Commun
2019 Apr 2;511(2):387-393. PMID: 30797555
Alogliptin purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Apr 2;511(2):387-393. [Abstract]
Western blotting analyses for TGF-b-induced phosphorylated Smad2/3 for Smad pathway, and phosphorylated Akt for non-Smad pathways and the effect of Alogliptin treatment.
-
-
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
-
Data Sheet (278 KB)
-
SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
-
Handling Instructions (2659 KB)
Verweise
[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]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.9464 mL | 14.7319 mL | 29.4638 mL | 73.6596 mL |
| 5 mM | 0.5893 mL | 2.9464 mL | 5.8928 mL | 14.7319 mL | |
| 10 mM | 0.2946 mL | 1.4732 mL | 2.9464 mL | 7.3660 mL | |
| 15 mM | 0.1964 mL | 0.9821 mL | 1.9643 mL | 4.9106 mL | |
| 20 mM | 0.1473 mL | 0.7366 mL | 1.4732 mL | 3.6830 mL | |
| 25 mM | 0.1179 mL | 0.5893 mL | 1.1786 mL | 2.9464 mL | |
| DMSO | 30 mM | 0.0982 mL | 0.4911 mL | 0.9821 mL | 2.4553 mL |
| 40 mM | 0.0737 mL | 0.3683 mL | 0.7366 mL | 1.8415 mL | |
| 50 mM | 0.0589 mL | 0.2946 mL | 0.5893 mL | 1.4732 mL | |
| 60 mM | 0.0491 mL | 0.2455 mL | 0.4911 mL | 1.2277 mL | |
| 80 mM | 0.0368 mL | 0.1841 mL | 0.3683 mL | 0.9207 mL | |
| 100 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7366 mL |
* 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.
Alogliptin Related Classifications
HY-A0023A Related Classifications
Powered by Bioz