General
Preferred name
SAXAGLIPTIN
Synonyms
Saxagliptin ()
SAXAGLIPTIN HYDRATE ()
Onglyza hydrate ()
BMS-477118 hydrate ()
SAXAGLIPTIN HYDROCHLORIDE ()
Saxagliptin (BMS-477118) ()
SAXAGLIPTIN ANHYDROUS ()
Oximidine II ()
Saxagliptin (hydrate) ()
Saxagliptin (hydrochloride) ()
BMS-477118 ()
BMS-477118 (hydrate) ()
BMS-477118 (hydrochloride) ()
Onglyza,BMS-477118 ()
BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate ()
SBMS-477118 ()
Saxagliptin monohydrate ()
Saxagliptine ()
BMS-477118-11 ()
Saxagliptin hydrate ()
Saxagliptin component of qternmet ()
NSC-760407 ()
Saxagliptina ()
Saxagliptin hydrochloride component of kombiglyze ()
Saxagliptin HCl ()
Saxagliptin hydrochloride component of qternmet xr ()
Saxagliptin hydrochloride component of qtern ()
Onglyza ()
Saxagliptin-13C-d2 (hydrochloride) ()
SAXAGLIPTIN COMPONENT OF QTERNMET ()
SAXAGLIPTIN MONOHYDRATE ()
SAXAGLIPTINA ()
SAXAGLIPTINE ()
P&D ID
PD001122
CAS
945667-22-1
709031-78-7
361442-04-8
1073057-20-1
361442-05-9
2699827-95-5
Tags
available
covalent binder
drug
drug candidate
Approved by
EMA
FDA
First approval
2009
Drug indication
Discovery agent
Type-2 diabetes
polycystic ovary syndrome
type 2 diabetes mellitus
Drug Status
approved
investigational
Max Phase
3.0
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
ABSORPTION Following a 5 mg single oral dose of saxagliptin to healthy subjects, the mean plasma AUC values for saxagliptin and its active metabolite were 78 ng•h/mL and 214 ng•h/mL, respectively. The corresponding plasma Cmax values were 24 ng/mL and 47 ng/mL, respectively. Saxagliptin did not accumulate following repeated doses. The median time to maximum concentration (Tmax) following the 5 mg once daily dose was 2 hours for saxagliptin and 4 hours for its active metabolite.; Bioavailability, 2.5 - 50 mg dose = 67%
HALF-LIFE Saxagliptin = 2.5 hours;; 5-hydroxy saxagliptin = 3.1 hours;
DESCRIPTION The USAN refers to the monohydrate. Note that marketed formulations may contain saxagliptin hydrochloride PubChem CID 49800073. (GtoPdb)
MOA Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor antidiabetic for the treatment of type 2 diabetes. DPP-4 inhibitors are a class of compounds that work by affecting the action of natural hormones in the body called incretins. Incretins decrease blood sugar by increasing consumption of sugar by the body, mainly through increasing insulin production in the pancreas, and by reducing production of sugar by the liver. [Bristol-Myers Squibb Press Release]; DPP-4 is a membrane associated peptidase which is found in many tissues, lymphocytes and plasma. DPP-4 has two main mechanisms of action, an enzymatic function and another mechanism where DPP-4 binds adenosine deaminase, which conveys intracellular signals via dimerization when activated. Saxagliptin forms a reversible, histidine-assisted covalent bond between its nitrile group and the S630 hydroxyl oxygen on DPP-4. The inhibition of DPP-4 increases levels active of glucagon like peptide 1 (GLP-1), which inhibits glucagon production from pancreatic alpha cells and increases production of insulin from pancreatic beta cells.;
DESCRIPTION Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research[1][2][3].
DESCRIPTION Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research[1][2][3].
PRICE 45
DESCRIPTION Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research[1][2][3].
DESCRIPTION Saxagliptin is a dipeptidyl peptidase-4 inhibitor. It is an antidiabetic drug used for the treatment of type 2 diabetes. (Enamine Bioactive Compounds)
DESCRIPTION Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM). (TargetMol Bioactive Compound Library)
DESCRIPTION Potent flap endonuclease 1 (FEN1) inhibitor; induces DNA damage response (Tocris Bioactive Compound Library)
DESCRIPTION Saxagliptin is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP-4). It has been approved for the treatment of type 2 diabetes. It was shown to prevent the inactivation of the incretin hormones GLP-1 and glucose-dependent insulinotropic polypeptide, thus promoting insulin secretion. (BOC Sciences Bioactive Compounds)
Compound Sets
31
AdooQ Bioactive Compound Library
A11109
BOC Sciences Bioactive Compounds
saxagliptin-hcl-salt-cas-709031-78-7-item-149517
Cayman Chemical Bioactives
23697
26709
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
CHEMBL385517
CHEMBL1201743
ChEMBL Drugs
CHEMBL385517
CHEMBL2103745
CHEMBL1201743
Concise Guide to Pharmacology 2017/18
6316
Concise Guide to Pharmacology 2019/20
6316
Concise Guide to Pharmacology 2021/22
6316
Concise Guide to Pharmacology 2023/24
6316
CovalentInDB
CI004947
CZ-OPENSCREEN Bioactive Library
DrugBank
DB06335
DrugBank Approved Drugs
DB06335
DrugCentral
4114
DrugCentral Approved Drugs
4114
DrugMAP
DMGXENV
DMW6K80
DrugMAP Approved Drugs
DMGXENV
Enamine Bioactive Compounds
EBC-02059
Enamine BioReference Compounds
EUbOPEN Chemogenomics Library
EUB0002710
Guide to Pharmacology
6316
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL385517
CHEMBL2103745
MedChem Express Bioactive Compound Library
HY-10285
HY-10285A
HY-16448
NCATS Inxight Approved Drugs
8I7IO46IVQ
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
Saxagliptin(Onglyza)
saxagliptin-hydrate
TargetMol Bioactive Compound Library
T0178
The Spectrum Collection
Tocris Bioactive Compound Library
6507
External IDs
66
Properties
(calculated by RDKit )
Molecular Weight
315.19
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
6
Aromatic Ring Count
0
cLogP
1.16
TPSA
90.35
Fraction CSP3
0.89
Chiral centers
6.0
Largest ring
6.0
QED
0.8
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
MOA
dipeptidyl peptidase 4 inhibitor
Inhibitor
Dipeptidyl Peptidase IV (CD26
DPP-IV
DP-IV) Inhibitors
Target
Dipeptidyl peptidase IV
Dipeptidyl Peptidase
DPP-4
DPP
Primary Target
Dipeptidyl Peptidase IV
Member status
member
Pathway
Metabolic Enzyme/Protease
Proteases/Proteasome
Ubiquitination
Recommended Cell Concentration
None
Source data