Saxagliptin hydrochloride
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.
- InChI
- InChI=1/C18H25N3O2.ClH/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;1H/t10?,11?,12-,13+,14+,15-,17?,18?;/s3
- 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
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Saxagliptin hydrochloride(709031-78-7)Related Product Information
- Carboxymethoxylamine hemihydrochloride
- BOC-DL-PROLINE ETHYL ESTER
- (1R,3S,5R)-2-AZABICYCLO[3.1.0]HEXANE-3-CARBOXAMIDE 2,2,2-TRIFLUOROACETIC ACID
- (1S,3R,5S)-2-tert-Butyl 3-ethyl 2-azabicyclo[3.1.0]hexane-2,3-dicarboxylate
- 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-aMino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1R,3R,5R)-
- 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-aMino-2-tricyclo[3.3.1.13,7]dec-1-ylacetyl]-, (1S,3S,5S)-
- 1H-Pyrrole-1-carboxylic acid, 2-(aMinocarbonyl)-2,3-dihydro-, 1,1-diMethylethyl ester, (2S)-
- (S) - N- Boc- adamantylglycine
- (S)-1-Boc-2,3-dihydro-2-pyrrolecarboxylic acid ethyl ester
- 2-Azabicyclo[3.1.0]hexane-2,3-dicarboxylic acid, 2-(1,1-dimethylethyl) 3-ethyl ester, (1S,3S,5S)-
- N-Boc-L-trans-4,5-Methanoproline
- (2R)-1,2-Pyrrolidinedicarboxylic acid 1-tert-butyl 2-ethyl ester
- (1S,3S,5S)-2-(TERT-BUTOXYCARBONYL)-2-AZABICYCLO[3.1.0]HEXANE-3-CARBOXYLIC ACID
- DSLXQSYLYSTVKT-ONZQNKQFSA-N
- 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-aMino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3R,5S)-
- Saxagliptin O-β-D-glucuronide
- 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-aMino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1R,3S,5R)-
- N-Boc-L-trans-4,5-methanoproline ethyl ester