Saxagliptin |
| Catalog No.GC12895 |
삭사글립틴(BMS-477118)은 강력하고 선택적이고 가역적이며 경쟁적이며 경구 활성인 디펩티딜 펩티다제-4(DPP-4)(Ki = 0.6-1.3nM) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 361442-04-8
Sample solution is provided at 25 µL, 10mM.
Saxagliptin is a highly potent dipeptidyl peptidase-4 (DPP-4) inhibitor that regulates blood glucose by selectively inhibiting the DPP-4 enzyme, thereby elevating levels of endogenous glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)[1-2]. Saxagliptin is used to improve glycemic control in patients with type II diabetes[3], and has been shown to alleviate inflammation and oxidative stress [4].
In vitro, treatment of human papillary thyroid carcinoma cell lines K1 and TPC-1 with Saxagliptin (0.1μM) for 24h significantly enhanced cell migration and invasion capabilities[5]. Pretreatment of human dental pulp cells with Saxagliptin (500nM–1μM) for 24–48 h, followed by stimulation with LPS (100ng/ml) for 24–48h, significantly suppressed the expression and secretion of pro-inflammatory cytokines TNF-α, IL-1β, and IL-8, while reducing inflammatory responses[6].
In vivo, oral administration of Saxagliptin (10mg/kg) once daily to a high-fat diet combined with streptozotocin (STZ; 50mg/kg)-induced type 2 diabetic C57BL/6J mouse model significantly improved β-cell mass and islet morphology, regardless of whether intervention began 7 days before or 1 day after STZ injury[7]. In another study, daily oral administration of Saxagliptin (10mg/kg) for 35 days to STZ (60mg/kg/day)-induced diabetic C57BL/6J mice markedly attenuated diabetes-induced somatic chromosomal instability. Saxagliptin significantly reduced the frequency of micronucleus formation in bone marrow and reversed diabetes-induced suppression of bone marrow nucleated cell proliferation[8].
References:
[1] Thareja S, Aggarwal S, Malla P, et al. Saxagliptin: a new drug for the treatment of type 2 diabetes. Mini Rev Med Chem. 2010 Jul;10(8):759-65.
[2] Kania DS, Gonzalvo JD, Weber ZA. Saxagliptin: a clinical review in the treatment of type 2 diabetes mellitus. Clin Ther. 2011 Aug;33(8):1005-22.
[3] Scirica BM, Bhatt DL, Braunwald E, et al. Saxagliptin and cardiovascular outcomes in patients with type 2 diabetes mellitus. N Engl J Med. 2013 Oct 3;369(14):1317-26.
[4] Zhang L, Qi X, Zhang G, et al. Saxagliptin protects against hypoxia-induced damage in H9c2 cells. Chem Biol Interact. 2020 Jan 5;315:108864.
[5] He L, Zhang T, Sun W, et al. The DPP-IV inhibitor saxagliptin promotes the migration and invasion of papillary thyroid carcinoma cells via the NRF2/HO1 pathway. Med Oncol. 2020 Oct 1;37(11):97.
[6] Guo X, Chen J. The protective effects of saxagliptin against lipopolysaccharide (LPS)-induced inflammation and damage in human dental pulp cells. Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):1288-1294.
[7] Poucher SM, Cheetham S, Francis J, et al. Effects of saxagliptin and sitagliptin on glycaemic control and pancreatic β-cell mass in a streptozotocin-induced mouse model of type 2 diabetes. Diabetes Obes Metab. 2012 Oct;14(10):918-26.
[8] Attia SM, Ahmad SF, Nadeem A, et al. Saxagliptin, a selective dipeptidyl peptidase-4 inhibitor, alleviates somatic cell aneugenicity and clastogenicity in diabetic mice. Mutat Res Genet Toxicol Environ Mutagen. 2023 Nov-Dec;892:503707.
| Cell experiment [1]: | |
Cell lines | K1 and TPC-1 human papillary thyroid carcinoma cell lines |
Preparation Method | Cells were cultured in RPMI 1640 or DMEM supplemented with 10% fetal bovine serum at 37°C, 5% CO₂. Cells were treated with Saxagliptin at a pharmacologically relevant concentration (0.1μM) for 24 hours in serum-free medium. |
Reaction Conditions | 0.1μM; 24h |
Applications | Saxagliptin significantly enhanced the migratory and invasive abilities of thyroid carcinoma cells, as demonstrated by Transwell assays. Saxagliptin upregulated the protein levels of MMP2 and VEGF, key mediators of metastasis. Saxagliptin also promoted nuclear and cytoplasmic accumulation of NRF2, activating the NRF2/HO1 pathway, which was essential for the observed pro-invasive effects. Silencing NRF2 abolished these changes, confirming the pathway's role. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Diabetes was induced by intraperitoneal injection of streptozotocin (60mg/kg/day for five consecutive days). Diabetic and non-diabetic mice were orally administered Saxagliptin (10mg/kg) once daily for 35 days. Bone marrow cells were collected 24 hours after the last treatment for micronucleus and oxidative stress analysis. |
Dosage form | 10mg/kg; oral gavage; once daily for 35 days. |
Applications | Saxagliptin significantly reduced the frequency of micronucleated polychromatic erythrocytes in diabetic mice, indicating protection against chromosomal instability. Fluorescence in situ hybridization revealed that Saxagliptin decreased both centromere-positive (aneugenic) and centromere-negative (clastogenic) micronuclei. Saxagliptin also restored redox balance by reducing lipid peroxidation (malondialdehyde levels) and increasing the reduced/oxidized glutathione ratio in bone marrow cells. Saxagliptin exhibited no mutagenic or cytotoxic effects in non-diabetic mice. |
References: | |
| Cas No. | 361442-04-8 | SDF | |
| Chemical Name | (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile | ||
| Canonical SMILES | C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N | ||
| Formula | C18H25N3O2 | M.Wt | 315.41 |
| Solubility | ≥ 14.85mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL |
| 5 mM | 634.1 μL | 3.1705 mL | 6.341 mL |
| 10 mM | 317 μL | 1.5852 mL | 3.1705 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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