| Identification | Back Directory | [Name]
Saxagliptin hydrochloride | [CAS]
709031-78-7 | [Synonyms]
Saxaint-S
Saxagliptin HCL salt
Saxagliptin hydrochloride
(1S,3S,5S)-2-[(2S)-Amino(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrochloride
(1S,3S,5S)-2-[(2S)-Amino(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile monohydrochloride | [EINECS(EC#)]
696-124-3 | [Molecular Formula]
C18H25N3O2.HCl | [MDL Number]
MFCD22572334 | [MOL File]
709031-78-7.mol | [Molecular Weight]
351.88 |
| Chemical Properties | Back Directory | [Melting point ]
>219°C | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (20 mg/ml) | [form ]
solid | [color ]
White | [Stability:]
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | [InChIKey]
TUAZNHHHYVBVBR-PMEPUXBANA-N | [SMILES]
[C@@H](C12CC3CC(CC(C3)(O)C1)C2)(N)C(N1[C@@H](C[C@@H]2C[C@H]12)C#N)=O.Cl |&1:0,15,17,19,r| |
| Hazard Information | Back Directory | [Description]
Saxagliptin (709031-78-7) is a clinically useful DPPIV inhibitor for the treatment of diabetes.1 ?Human DPP-IV Ki = 0.6 nM.2 | [Uses]
Saxagliptin is a potent and selective reversible inhibitor of dipeptidyl peptidase-4, which is being developed for the treatment of type 2 diabetes. It is absorbed rapidly after oral administration and has a pharmacokinetic profile compatible with once daily dosing. | [in vivo]
Saxagliptin (1 mg/kg; for 12 weeks) treatment in high-fat diet/streptozotocin-induced diabetic rats, significant improvement in pancreas insulin secretion capacity evaluated by hyperglycemia clamp and increased β-cell to α-cell areas ratio are observed[1].
Saxagliptin dose-dependently inhibits plasma DPP-4 activity in Han-Wistar rats, by ~70% at 7 hours postdose with 1 mg/kg and by ~90% at 7 hours postdose with 10 mg/kg. At 24 hours postdose, ~20% and 70% inhibition, respectively, remained[2]. | [IC 50]
DPP-4 | [storage]
Store at -20°C | [References]
Tahrani et al. (2009) Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus; Adv. Ther. 26 249
Augeri et al. (2005) Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes; J. Med. Chem. 48 5025 |
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