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| | Saxagliptin hydrochloride Basic information |
| Product Name: | Saxagliptin hydrochloride | | Synonyms: | 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 monohydrochloride;(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;Saxagliptin HCL salt;Saxaint-S;2-Azabicyclo[3.1.0]hexane-3-carbonitrile,2-[(2S)-amino(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-,monohydrochloride, (1S,3S,5S)- | | CAS: | 709031-78-7 | | MF: | C18H25N3O2.HCl | | MW: | 351.88 | | EINECS: | 696-124-3 | | Product Categories: | Saxagliptin Hydrochloride | | Mol File: | 709031-78-7.mol |  |
| | Saxagliptin hydrochloride Chemical Properties |
| 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| |
| | Saxagliptin hydrochloride Usage And Synthesis |
| 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 | [1] ABD A. TAHRANI Anthony H B Milan K Piya. Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus[J]. Advances in Therapy, 2009, 26 3: 249-262. DOI:10.1007/s12325-009-0014-9
[2] DAVID J. AUGERI. 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]. Journal of Medicinal Chemistry, 2005, 48 15: 5025-5037. DOI:10.1021/jm050261p |
| | Saxagliptin hydrochloride Preparation Products And Raw materials |
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