| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
Saxagliptin (formerly also known as BMS-477118; brand name: Onglyza) is a potent, orally bioactive, selective and reversible DPP-4 (dipeptidyl peptidase-4) inhibitor with potential anti-hyperglycemic activity. With an IC50 of 26 nM, it inhibits DPP-4. The FDA authorized saxagliptin in 2008 for the management of type 2 diabetes. Saxagliptin inhibits ERK phosphorylation and cell proliferation in vitro in MSC and MC3T3E1 preosteoblasts, as well as in response to FBS, insulin, and IGF1. Without growth factors, saxagliptin has no effect on cell proliferation or ERK activation.
| Targets |
DPP-4 (IC50 = 26 nM)
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|---|---|
| ln Vitro |
Saxagliptin has a DPP4 inhibition constant Ki of 1.3 nM, making it ten times more potent than sitagliptin and vildagliptin, two other DPP4 inhibitors, with Ki values of 13 and 18 nM, respectively. Furthermore, saxagliptin exhibits 400- and 75-fold higher specificity for DPP4 than it does for DPP8 or DPP9. Saxagliptin's active metablite has twice the potency of the parent drug. When compared to various other proteases, saxagliptin and its metabolite are both highly selective (>4000-fold) for preventing DPP4 (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9).[2] Saxagliptin is linked to better β-cell function, suppression of glucagon secretion, and decreased degradation of the incretin hormone glucagon-like peptide-1, which enhances its actions.[3]
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| ln Vivo |
Maximum Saxagliptin responses in glucose excursion in Zuckerfa/fa rats are correlated with plasma DPP4 inhibition of about 60% compared to control; at higher percent inhibition, no further antihyperglycemic effects are observed. In the dosage range of 0.13-1.3 mg/kg, saxagliptin significantly increases glucose clearance in ob/ob mice compared to controls in a dose-dependent manner. When saxagliptin is taken in a dose-dependent manner, it significantly raises plasma insulin at 15 minutes after the glucose tolerance test (GTT) and simultaneously improves the glucose clearance curves 60 minutes later.[4]
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| Enzyme Assay |
saxagliptin H2O (BMS477118 H2O) is a reversible and selective DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.
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| Animal Protocol |
Male 13−14 week-old ob/ob mice
10 μmol/kg Orally |
| References |
| Molecular Formula |
C18H25N3O2
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|---|---|
| Molecular Weight |
315.41
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| Exact Mass |
315.19
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| Elemental Analysis |
C, 68.54; H, 7.99; N, 13.32; O, 10.14
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| CAS # |
361442-04-8
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| Related CAS # |
Saxagliptin hydrate;945667-22-1;Saxagliptin hydrochloride;709031-78-7
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| Appearance |
Solid powder
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| SMILES |
C1[C@@H]2C[C@@H]2N([C@@H]1C#N)C(=O)[C@H](C34CC5CC(C3)CC(C5)(C4)O)N
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| InChi Key |
QGJUIPDUBHWZPV-SGTAVMJGSA-N
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| InChi Code |
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
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| Chemical Name |
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
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| Synonyms |
BMS 477118; Saxagliptin; BMS-477118; BMS477118; brand name: Onglyza
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 8.33 mg/mL (26.41 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
Solubility in Formulation 2: Saline: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL | |
| 5 mM | 0.6341 mL | 3.1705 mL | 6.3410 mL | |
| 10 mM | 0.3170 mL | 1.5852 mL | 3.1705 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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