Saxagliptin (BMS-477118)

Catalog No.S1540 Batch:S154002

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Technical Data

Formula

C18H25N3O2
Molecular Weight 315.41 CAS No. 361442-04-8
Solubility (25°C)* In vitro DMSO 63 mg/mL (199.74 mM)
Water 63 mg/mL (199.74 mM)
Ethanol 63 mg/mL (199.74 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Targets
DPP-4 [1]
26 nM
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. [3]
In vivo Maximal responses of Saxagliptin in glucose excursion in Zuckerfa/fa rats are associated with plasma DPP4 inhibition of approximately 60% vs. control, and no additional antihyperglycemic effects are seen at higher percent inhibition. 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]

Protocol (from reference)

Animal Study:[4]
  • Animal Models

    Male 13−14 week-old ob/ob mice

  • Dosages

    10 μmol/kg

  • Administration

    Orally

Customer Product Validation

Data from [Data independently produced by , , J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1081-1082:109-117]

Selleck's Saxagliptin (BMS-477118) has been cited by 5 publications

Simultaneous Estimation of Saxagliptin and Dapagliflozin in Human Plasma by Validated High Performance Liquid Chromatography - Ultraviolet Method [ Turk J Pharm Sci, 2019, 16(2):227-233] PubMed: 32454718
Subversion of Systemic Glucose Metabolism as a Mechanism to Support the Growth of Leukemia Cells. [ Cancer Cell, 2018, 34(4):659-673] PubMed: 30270124
Sensitive analysis and pharmacokinetic study of a novel gemcitabine carbamate prodrug and its active metabolite gemcitabine in rats using LC-ESI-MS/MS [Zhou Y, et al. J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257] PubMed: 29554521
Quantitative determination of metformin, saxagliptin and 5-hydroxy saxagliptin simultaneously by hydrophilic interaction liquid chromatography - electrospray ionization mass spectrometry and its application to a bioequivalence study with a single-pill com䲧盌Ỵ盍㧀盋膉甘 [Peng Y, et al. J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1081-1082:109-117] PubMed: 29518719
Molecular cloning and biochemical characterization of Xaa-Pro dipeptidyl-peptidase from Streptococcus mutans and its inhibition by anti-human DPP IV drugs. [ FEMS Microbiol Lett, 2016, 363(9)] PubMed: 27010012

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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