SaxagliptinSelective DPP4 inhibitor CAS# 361442-04-8 |
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Quality Control & MSDS
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| Cas No. | 361442-04-8 | SDF | Download SDF |
| PubChem ID | 11243969 | Appearance | Powder |
| Formula | C18H25N3O2 | M.Wt | 315.41 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | BMS-477118 | ||
| Solubility | DMSO : ≥ 34 mg/mL (107.80 mM) H2O : 10 mg/mL (31.70 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile | ||
| SMILES | C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N | ||
| Standard InChIKey | QGJUIPDUBHWZPV-SGTAVMJGSA-N | ||
| Standard InChI | InChI=1S/C18H25N3O2/c19-8-13-2-12-3-14(12)21(13)16(22)15(20)17-4-10-1-11(5-17)7-18(23,6-10)9-17/h10-15,23H,1-7,9,20H2/t10?,11?,12-,13+,14+,15-,17?,18?/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Saxagliptin(BMS477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.
IC50 value: 26 nM [1]
Target: DPP4
in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.
in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4]. References: | |||||
Saxagliptin Dilution Calculator
Saxagliptin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL | 63.4095 mL | 79.2619 mL |
| 5 mM | 0.6341 mL | 3.1705 mL | 6.341 mL | 12.6819 mL | 15.8524 mL |
| 10 mM | 0.317 mL | 1.5852 mL | 3.1705 mL | 6.341 mL | 7.9262 mL |
| 50 mM | 0.0634 mL | 0.317 mL | 0.6341 mL | 1.2682 mL | 1.5852 mL |
| 100 mM | 0.0317 mL | 0.1585 mL | 0.317 mL | 0.6341 mL | 0.7926 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Saxagliptin is a drug which was developed for the treatment of respiratory disorders such as asthma and Chronic Obstructive Pulmonary Disease (COPD). It is orally active and acts as a selective Phosphodiesterase-4 inhibitor.
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Efficacy and safety of saxagliptin compared with acarbose in Chinese patients with type 2 diabetes mellitus uncontrolled on metformin monotherapy: Results of a Phase IV open-label randomized controlled study (the SMART study).[Pubmed:28296055]
Diabetes Obes Metab. 2017 Nov;19(11):1513-1520.
AIM: To investigate the efficacy, safety and tolerability of Saxagliptin compared with acarbose in Chinese patients with type 2 diabetes mellitus inadequately controlled with metformin monotherapy. METHODS: SMART was a 24-week, multicentre, randomized, parallel-group, open-label Phase IV study conducted at 35 sites in China (September 24, 2014 to September 29, 2015). The primary outcome was absolute change from baseline in HbA1c at Week 24. Secondary outcomes assessed at Week 24 included the proportion of patients achieving HbA1c < 7.0%, the proportion of patients with gastrointestinal adverse events (GI AEs), and the proportion of patients achieving HbA1c < 7.0% without GI AEs. Safety and tolerability were also assessed in all patients who received >/=1 dose of study medication. RESULTS: Four-hundred and eighty-eight patients were randomized (1:1) to Saxagliptin or acarbose via a central randomization system (interactive voice/web response system); 241 and 244 patients received Saxagliptin and acarbose, respectively, and 238 and 243 of these had >/=1 pre- and >/=1 post-baseline efficacy values recorded. Saxagliptin was non-inferior to acarbose for glycaemic control [Week 24 HbA1c change: -0.82% and -0.78%, respectively; difference (95% confidence interval): -0.04 (-0.22, 0.13)%], with similar proportions of patients in both treatment groups achieving HbA1c < 7.0%. However, fewer GI AEs were reported with Saxagliptin compared with acarbose, and a greater number of patients who received Saxagliptin achieved HbA1c < 7.0% without GI AEs compared with those receiving acarbose. CONCLUSION: Both therapies had similar efficacy profiles. However, Saxagliptin was associated with fewer GI AEs, suggesting it might be preferential for clinical practice. CLINICAL TRIAL REGISTRATION NUMBER: NCT02243176, clinicaltrials.gov.
Pharmacokinetic drug evaluation of saxagliptin plus dapagliflozin for the treatment of type 2 diabetes.[Pubmed:28374622]
Expert Opin Drug Metab Toxicol. 2017 May;13(5):583-592.
INTRODUCTION: Combining a dipeptidyl peptidase-4 inhibitor and a sodium-glucose cotransporter type 2 inhibitor is an attractive option to treat hyperglycaemia in type 2 diabetes. Areas covered: The Saxagliptin plus dapagliflozin combination is carefully analysed, focusing on: 1) pharmacokinetic properties, 2) pharmacodynamics data, and 3) results of randomised controlled trials (dual combination versus either monotherapy, sequential therapy Saxagliptin added to dapagliflozin or dapagliflozin added to Saxagliptin). Expert opinion: Pharmacokinetic findings demonstrate the absence of drug-drug interaction and the bioequivalence of the FDC compared with separated tablets. Pharmacodynamic observations confirm a complementary mode of action of the two agents. Dual Saxagliptin-dapagliflozin therapy is more potent than either monotherapy. It may be used as an initial combination, although this approach remains debatable and should probably be reserved in case of high glycated hemoglobin, or a stepwise strategy, according to a personalized approach. The developed Saxagliptin-dapagliflozin FDC may simplify anti-hyperglycemic therapy and improve drug compliance.
