- Cat. No.
- A11109
Saxagliptin (BMS-477118)
Synonyms: BMS-477118; Onglyza
Saxagliptin (BMS-477118) is a new dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 50 nM.
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Dipeptidyl peptidase 4 (DPP-4) inhibitors block a serine protease that trims dipeptides from incretin hormones. DPP-4, also known as cluster of differentiation 26 (CD26), prefers substrates with proline or alanine at the second position. In 1993 it was shown to cleave glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) and to account for their degradation in human serum. Inhibiting the enzyme therefore prolongs incretin signaling in studies of glucose homeostasis and insulin secretion. Sitagliptin, alogliptin benzoate and linagliptin bind to the active site without forming a covalent bond. Vildagliptin and saxagliptin are cyanopyrrolidines that form a reversible covalent adduct with the catalytic serine. Trelagliptin and gemigliptin add further gliptin scaffolds for structure-activity comparisons.
Synonyms: BMS-477118; Onglyza
Saxagliptin (BMS-477118) is a new dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 50 nM.
Synonyms: MK-0431
Sitagliptin is an oral antihyperglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class.
Synonyms: BI-1356; Tradjenta; Trajenta
Linagliptin is a DPP-4 inhibitor, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).
Vildagliptin is a dipeptidyl peptidase-4 (CD26) inhibitor.
Synonyms: SYR-472
Trelagliptin is a highly selective, long-acting DPP-4 inhibitor.
Gemigliptin is a highly selective dipeptidyl peptidase 4 (DPP4) inhibitor with a KD of 7.25 nM.
Synonyms: Januvia; MK-0431
Sitagliptin phosphate is an anti-diabetic (antihyperglycemic) drug of the dipeptidyl peptidase-4 (DPP-4) class. Inhibition of the enzyme DPP-4 is thought to increase Glucagon-like peptide-1 (GLP-1) which inhibits glucagon release , stimulates the insulin release and lowers blood glucose.
Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
Synonyms: SYR-322; Nesina
Alogliptin Benzoate is a dipeptidyl-peptidase-4 (DPP 4) inhibitor
Synonyms: SYR472; SYR 111472
Trelagliptin is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).
Synonyms: SK-0403
Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM); > 10 fold less potent for DPP-8 and DPP-9.
Synonyms: SYR-322; Axagliptin hydrate
Alogliptin is a potent, selective inhibitor of DPP-4 with IC50 of
DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
Synonyms: Val-boroPro; PT100
Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM).
Talabostat mesylate is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.
Synonyms: Dipeptidylpeptidase IV Inhibitor III
DPPI 1c hydrochloride is a dicyanopyrrolidine compound that acts as a slow-binding and active site-targeting inhibitor of CD26 (DPP 4), with an IC50 = 106 nM and little activity against DPP II, DPP III, DPP VIII, DPP IX, FAP, or APP even at concentrations as high as 30 μM.
PK 44 phosphate is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an IC50 value of 15.8 nM.
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NVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV with Ki and IC50 values of 11 nM and 14 nM, respectively.
Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.
UAMC 00039 dihydrochloride is a potent inhibitor of dipeptidyl peptidase II (DPP-II) (IC50 = 0.48 nM). Exhibits selectivity for DPP-II against DPP-9, DPP-8 and DPP-IV (IC50 values are 78.6, 142 and 165 μM, respectively).
Synonyms: BMS-477118 hydrate
Saxagliptin H2O(BMS477118 H2O) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.
Synonyms: INS 1007
AZD7986, also known as INS 1007, is a second generation reversible covalent, potent and selective DPP1 inhibitor potentially for the treatment of chronic obstructive pulmonary disease (COPD) with predicted human PK properties suitable for once daily human dosing.
Synonyms: SP 2086
Retagliptin Phosphate is pharmaceutical composition of DPP-4 inhibitor for treating type-2 diabetes.