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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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| 500mg |
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| 1g |
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Purity: ≥98%
Saxagliptin hydrate (also known as BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate; brand name: Onglyza), the hydrate form of Saxagliptin, is a potent, orally bioactive, selective and reversible, oral bioactive DPP4 (dipeptidyl peptidase-4) inhibitor with an IC50 of 26 nM. The FDA authorized saxagliptin in 2008 for the management of type 2 diabetes. In individuals with type 2 diabetes mellitus, saxagliptin, a competitive DPP4 inhibitor, decreases fasting and postprandial glucose concentrations in a glucose-dependent manner by delaying the inactivation of the incretin hormones. 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 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. In the presence of FBS, saxagliptin decreases the expression of Runx2 and osteocalcin, as well as the production and mineralization of type-1 collagen in MSC and MC3T3E1 cells, while elevating the expression of PPAR-gamma.
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| ln Vivo |
Saxagliptin increases NO availability and enhances antioxidant status, which directly benefits the arterial wall in an animal model of type 2 diabetes. Through the inhibition of NAD(P)H oxidase-driven eNOS uncoupling and the reduction of the action of cyclooxygenase-1-derived vasoconstrictors downregulating the expression of thromboxane-prostanoid receptors, saxagliptin reverses vascular hypertrophic remodeling and ameliorates NO availability in small arteries from db/db mice[2]. Moreover, pancreatic β-cell function is enhanced in both postprandial and fasting conditions by DPP-4 inhibition with saxagliptin, and postprandial glucagon concentration is reduced[3].
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| Enzyme Assay |
Saxagliptin H2O(BMS477118 H2O) has an IC50 of 26 nM and a Ki of 1.3 nM, making it a selective and reversible DPP4 inhibitor.
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| Cell Assay |
Once serum-starved for one night, sub-confluent cells are incubated with 1.5 or 15 μM saxagliptin, FBS (1%), insulin (5 ng/mL), or IGF1 (10-8 M) for either one hour (affecting signal transduction mechanisms) or twenty-four hours (affecting cell proliferation).
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| Animal Protocol |
adult mice C57BLKS/J; db/db mice
0.1 mg/kg p.o. |
| References |
| Molecular Formula |
C18H25N3O2.H2O
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|---|---|
| Molecular Weight |
333.43
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| Exact Mass |
315.19
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| Elemental Analysis |
C, 64.84; H, 8.16; N, 12.60; O, 14.39
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| CAS # |
945667-22-1
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| Related CAS # |
Saxagliptin;361442-04-8;Saxagliptin hydrochloride;709031-78-7
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| Appearance |
Off-white to light yellow 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.O
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| InChi Key |
AFNTWHMDBNQQPX-NHKADLRUSA-N
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| InChi Code |
InChI=1S/C18H25N3O2.H2O/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;1H2/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;hydrate
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| Synonyms |
BMS-477118 hydrate; Onglyza hydrate; BMS 477118 hydrate; BMS477118 hydrate; 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9991 mL | 14.9957 mL | 29.9913 mL | |
| 5 mM | 0.5998 mL | 2.9991 mL | 5.9983 mL | |
| 10 mM | 0.2999 mL | 1.4996 mL | 2.9991 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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