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Saxagliptin hydrochloride

Product NameSaxagliptin hydrochloride
CAS709031-78-7
MFC18H25N3O2.HCl
MW351.88
EINECS696-124-3
MOL File709031-78-7.mol

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\|

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

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