Saxagliptin
Based on 6 publication(s) in Google Scholar
Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research.
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- Pureza: 99.96%
- No. CAS: 361442-04-8
- Fòrmula: C18H25N3O2
- Peso molecular:315.41
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Publications Citing Use of MedChemExpress (MCE) Saxagliptin
More- Int J Biol Macromol. 2024 Oct;278(Pt 2):134783. [Abstract]
- Biochem Pharmacol. 2020 Jul:177:113951. [Abstract]
- J Mol Cell Cardiol. 2026 Jan 19:213:14-30. [Abstract]
- J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Abstract]
- Andrology. 2023 Feb;11(2):295-306. [Abstract]
- Front Oncol. 2021 Sep 24:11:728047. [Abstract]
Actividad biológica
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DPP-4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
50 nM
Compound: Saxagliptin
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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
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[PMID: 23623674] |
| U-87MG ATCC | IC50 |
1720 μM
Compound: Saxagliptin
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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
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[PMID: 32527554] |
Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation[1].
Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment increases the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression[1].
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:INS-1 832/13 cells
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Concentration:100 nM
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Incubation Time:48 hours
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Result:Significantly induced β-cell proliferation.
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Cell Line:INS-1 832/13 cells
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Concentration:100 nM
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Incubation Time:48 hours
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Result:Increased the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression.
Saxagliptin dose-dependently inhibits plasma DPP-4 activity in Han-Wistar rats, by ~70% at 7 hours postdose with 1 mg/kg and by ~90% at 7 hours postdose with 10 mg/kg. At 24 hours postdose, ~20% and 70% inhibition, respectively, remained[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 361442-04-8
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Appearance Solid
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Peso molecular 315.41
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Fòrmula C18H25N3O2
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Color White to off-white
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SMILES
N[C@@H]([C@](C[C@H](C1)C2)(C[C@@H]1C3)C[C@]23O)C(N([C@@H](C4)C#N)[C@@H]5[C@H]4C5)=O
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Synonyms
BMS-477118
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (6)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
An acidic polysaccharide promoting GLP-1 secretion from Dendrobium huoshanense protocorm-like bodies: Structure validation and activity exploration. [Abstract]2024 Oct;278(Pt 2):134783. PMID: 39153673 -
Biochem Pharmacol
Dipeptidyl peptidase-4 inhibition improves endothelial senescence by activating AMPK/SIRT1/Nrf2 signaling pathway. [Abstract]2020 Jul:177:113951. PMID: 32251672 -
J Mol Cell Cardiol
DPP4-regulated endothelial cell ferroptosis modulates atherosclerosis progression by ferritinophagy. [Abstract]2026 Jan 19:213:14-30. PMID: 41565199 -
J Biol Chem
Human DPP9 represses NLRP1 inflammasome and protects against autoinflammatory diseases via both peptidase activity and FIIND domain binding. [Abstract]2018 Dec 7;293(49):18864-18878. PMID: 30291141 -
Andrology
Saxagliptin alleviates erectile dysfunction through increasing stromal cell-derived factor-1 in diabetes mellitus. [Abstract]2023 Feb;11(2):295-306. PMID: 36113503 -
Front Oncol
Antidiabetic DPP-4 Inhibitors Reprogram Tumor Microenvironment That Facilitates Murine Breast Cancer Metastasis Through Interaction With Cancer Cells via a ROS-NF-кB-NLRP3 Axis. [Abstract]2021 Sep 24:11:728047. PMID: 34631556
Solvente y solubilidad
DMSO : ≥ 34 mg/mL (107.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 10 mg/mL (31.70 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 8.33 mg/mL (26.41 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Chun-Jun Li, et al. Saxagliptin Induces β-Cell Proliferation through Increasing Stromal Cell-Derived Factor-1α In Vivo and In Vitro. Front Endocrinol (Lausanne). 2017 Nov 27;8:326. [Content Brief]
[2]. Darshan J Dave. Saxagliptin: A dipeptidyl peptidase-4 inhibitor in the treatment of type 2 diabetes mellitus. J Pharmacol Pharmacother. 2011 Oct;2(4):230-5. [Content Brief]
[3]. Carolyn F Deacon, et al. Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Adv Ther. 2009 May;26(5):488-99. [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 (protect from light, stored under nitrogen). 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 | 3.1705 mL | 15.8524 mL | 31.7048 mL | 79.2619 mL |
| 5 mM | 0.6341 mL | 3.1705 mL | 6.3410 mL | 15.8524 mL | |
| 10 mM | 0.3170 mL | 1.5852 mL | 3.1705 mL | 7.9262 mL | |
| 15 mM | 0.2114 mL | 1.0568 mL | 2.1137 mL | 5.2841 mL | |
| 20 mM | 0.1585 mL | 0.7926 mL | 1.5852 mL | 3.9631 mL | |
| 25 mM | 0.1268 mL | 0.6341 mL | 1.2682 mL | 3.1705 mL | |
| 30 mM | 0.1057 mL | 0.5284 mL | 1.0568 mL | 2.6421 mL | |
| DMSO | 40 mM | 0.0793 mL | 0.3963 mL | 0.7926 mL | 1.9815 mL |
| 50 mM | 0.0634 mL | 0.3170 mL | 0.6341 mL | 1.5852 mL | |
| 60 mM | 0.0528 mL | 0.2642 mL | 0.5284 mL | 1.3210 mL | |
| 80 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9908 mL | |
| 100 mM | 0.0317 mL | 0.1585 mL | 0.3170 mL | 0.7926 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.
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