S5079 |
Sitagliptin
|
Sitagliptin (MK-0431) is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes. |
-
OPARU, 2024, 10.18725/OPARU-52005
-
Mol Biotechnol, 2023, 10.1007/s12033-023-00992-9
-
bioRxiv, 2023, 10.1101/2023.12.18.572126
|
|
S3033 |
Vildagliptin
|
Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM. |
-
Int J Mol Sci, 2024, 25(18)9760
-
J Clin Invest, 2023, 133(12)e165933
-
Oncoimmunology, 2023, 12(1):2268257
|
|
S4002 |
Sitagliptin phosphate monohydrate
|
Sitagliptin phosphate monohydrate (MK-0431) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts. |
-
Front Oncol, 2021, 11:704024
-
J Biomol Struct Dyn, 2021, 1-12
-
J Diabetes Res, 2020, 2020:2450781
|
|
S1540 |
Saxagliptin (BMS-477118)
|
Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
-
Turk J Pharm Sci, 2019, 16(2):227-233
-
Cancer Cell, 2018, 34(4):659-673
-
J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257
|
|
S8455 |
Talabostat (PT-100)
|
Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities. |
-
J Oral Microbiol, 2024, 16(1):2373040
-
Brain Res, 2024, S0006-8993(24)00383-4
-
Nat Chem Biol, 2023, 19(4):431-439
|
|
S9631 |
Puromycin aminonucleoside
|
Puromycin aminonucleoside (NSC 3056, PAN, Stylomycin aminonucleoside, ARDMA, SAN), the aminonucleoside portion of the antibiotic puromycin, is a reversible inhibitor of dipeptidyl-peptidase II and cytosol alanyl aminopeptidase that induces apoptosis in mesangial cells (MCs) accompanied by declined cell viability and enhanced inflammatory response. |
-
Cell Mol Biol Lett, 2023, 28(1):62
-
Cell Mol Biol Lett, 2023, 28(1):62
-
Oral Dis, 2022, 10.1111/odi.14321
|
|
S8565 |
Omarigliptin (MK-3102)
|
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). |
-
NYMC Student Theses and Dissertations, 2023,
-
Acta Pharmacol Sin, 2021, 1-9
-
Front Behav Neurosci, 2021, 15:705579
|
|
S2868 |
Alogliptin (SYR-322) benzoate
|
Alogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. |
-
Cell Rep, 2017, 20(7):1692-1704
|
|
S5365 |
Alogliptin
|
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. |
-
Sci Adv, 2021, 7(27)eabh3032
|
|
S4697 |
Saxagliptin hydrate
|
Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
-
Turk J Pharm Sci, 2019, 16(2):227-233
|
|
E3049 |
Lobeliae Chinensis Extract
|
Lobeliae Chinensis Extract is extracted from Lobeliae Chinensis, which is a traditional Chinese herb widely used in the treatment of diabetes and found to have a hypoglycaemic mechanism related to the inhibition of DPP4. |
|
|
E4814New |
Teneligliptin Hydrobromide Hydrate
|
Teneligliptin Hydrobromide Hydrate(MP-513 hydrobromide hydrate) is a potent, competitive, and long-lasting inhibitor of DPP-4. It competitively inhibited rhDPP-4, human plasma, and rat plasma with IC50 values of 0.889, 1.75, and 1.35 nM respectively. It suppresses high glucose-mediated mitochondrial dysfunction and can be used for treatment of type 2 diabetes. |
|
|
E1188New |
Brensocatib
|
Brensocatib (AZD7986, INS1007) is an oral, selective, reversible inhibitor of dipeptidyl peptidase-1 (DPP-1). It reduces the activity of all major neutrophil serine proteases (NSPs) including, neutrophil elastase (NE), proteinase 3 (PR3), and cathepsin G (CatG) in patients with bronchiectasis. |
-
Nat Commun, 2024, 15(1):6519
|
|
E4804New |
Sitagliptin phosphate
|
Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of dipeptidyl peptidase IV (DPP-4) with an IC50 value of 19 nM in Caco-2 cell extracts. |
|
|
S5909 |
Anagliptin
|
Anagliptin is an orally active and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor and exerts anti-inflammatory effects on macrophages, adipocytes, and mouse livers by suppressing NF-κB activation. |
|
|
E4916New |
Bestatin hydrochloride
|
Bestatin hydrochloride is an inhibitor of aminopeptidase N and enkephalinase that elevates the levels of angiotensin II and angiotensin III. It also acts as a non-competitive inhibitor (α > 1) of porcine DPP-IV with a Ki value of 75 μM. It reduces DPP-IV activity, decreases cell viability, and increases DNA fragmentation in vitro. It has the potential to treat skin conditions like acne, psoriasis and keloids. |
|
|
A2517 |
Begelomab (Anti-DPP4 / CD26)
|
Begelomab (Anti-DPP4 / CD26) is a monoclonal antibody targeting DPP-4/CD26. Begelomab can be used for the research of severe refractory idiopathic inflammatory myopathy. MW: 145.5 KD. |
|
|
S7513 |
Trelagliptin
|
Trelagliptin (SYR-472), a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM, improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM). |
|
|
S4636 |
Teneligliptin hydrobromide
|
Teneligliptin (Teneligliptin hydrobromide anhydrous) 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. |
|
|
S5063 |
Trelagliptin succinate
|
Trelagliptin succinate (SYR472) is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM). |
|
|
E0122 |
Gemigliptin
|
Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.
|
|
|
S5079 |
Sitagliptin
|
Sitagliptin (MK-0431) is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes. |
- OPARU, 2024, 10.18725/OPARU-52005
- Mol Biotechnol, 2023, 10.1007/s12033-023-00992-9
- bioRxiv, 2023, 10.1101/2023.12.18.572126
|
|
S3033 |
Vildagliptin
|
Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM. |
- Int J Mol Sci, 2024, 25(18)9760
- J Clin Invest, 2023, 133(12)e165933
- Oncoimmunology, 2023, 12(1):2268257
|
|
S4002 |
Sitagliptin phosphate monohydrate
|
Sitagliptin phosphate monohydrate (MK-0431) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts. |
- Front Oncol, 2021, 11:704024
- J Biomol Struct Dyn, 2021, 1-12
- J Diabetes Res, 2020, 2020:2450781
|
|
S1540 |
Saxagliptin (BMS-477118)
|
Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
- Turk J Pharm Sci, 2019, 16(2):227-233
- Cancer Cell, 2018, 34(4):659-673
- J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257
|
|
S8455 |
Talabostat (PT-100)
|
Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities. |
- J Oral Microbiol, 2024, 16(1):2373040
- Brain Res, 2024, S0006-8993(24)00383-4
- Nat Chem Biol, 2023, 19(4):431-439
|
|
S9631 |
Puromycin aminonucleoside
|
Puromycin aminonucleoside (NSC 3056, PAN, Stylomycin aminonucleoside, ARDMA, SAN), the aminonucleoside portion of the antibiotic puromycin, is a reversible inhibitor of dipeptidyl-peptidase II and cytosol alanyl aminopeptidase that induces apoptosis in mesangial cells (MCs) accompanied by declined cell viability and enhanced inflammatory response. |
- Cell Mol Biol Lett, 2023, 28(1):62
- Cell Mol Biol Lett, 2023, 28(1):62
- Oral Dis, 2022, 10.1111/odi.14321
|
|
S8565 |
Omarigliptin (MK-3102)
|
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). |
- NYMC Student Theses and Dissertations, 2023,
- Acta Pharmacol Sin, 2021, 1-9
- Front Behav Neurosci, 2021, 15:705579
|
|
S2868 |
Alogliptin (SYR-322) benzoate
|
Alogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. |
- Cell Rep, 2017, 20(7):1692-1704
|
|
S5365 |
Alogliptin
|
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. |
- Sci Adv, 2021, 7(27)eabh3032
|
|
S4697 |
Saxagliptin hydrate
|
Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
- Turk J Pharm Sci, 2019, 16(2):227-233
|
|
E3049 |
Lobeliae Chinensis Extract
|
Lobeliae Chinensis Extract is extracted from Lobeliae Chinensis, which is a traditional Chinese herb widely used in the treatment of diabetes and found to have a hypoglycaemic mechanism related to the inhibition of DPP4. |
|
|
E4814New |
Teneligliptin Hydrobromide Hydrate
|
Teneligliptin Hydrobromide Hydrate(MP-513 hydrobromide hydrate) is a potent, competitive, and long-lasting inhibitor of DPP-4. It competitively inhibited rhDPP-4, human plasma, and rat plasma with IC50 values of 0.889, 1.75, and 1.35 nM respectively. It suppresses high glucose-mediated mitochondrial dysfunction and can be used for treatment of type 2 diabetes. |
|
|
E1188New |
Brensocatib
|
Brensocatib (AZD7986, INS1007) is an oral, selective, reversible inhibitor of dipeptidyl peptidase-1 (DPP-1). It reduces the activity of all major neutrophil serine proteases (NSPs) including, neutrophil elastase (NE), proteinase 3 (PR3), and cathepsin G (CatG) in patients with bronchiectasis. |
- Nat Commun, 2024, 15(1):6519
|
|
E4804New |
Sitagliptin phosphate
|
Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of dipeptidyl peptidase IV (DPP-4) with an IC50 value of 19 nM in Caco-2 cell extracts. |
|
|
S5909 |
Anagliptin
|
Anagliptin is an orally active and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor and exerts anti-inflammatory effects on macrophages, adipocytes, and mouse livers by suppressing NF-κB activation. |
|
|
E4916New |
Bestatin hydrochloride
|
Bestatin hydrochloride is an inhibitor of aminopeptidase N and enkephalinase that elevates the levels of angiotensin II and angiotensin III. It also acts as a non-competitive inhibitor (α > 1) of porcine DPP-IV with a Ki value of 75 μM. It reduces DPP-IV activity, decreases cell viability, and increases DNA fragmentation in vitro. It has the potential to treat skin conditions like acne, psoriasis and keloids. |
|
|
S7513 |
Trelagliptin
|
Trelagliptin (SYR-472), a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM, improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM). |
|
|
S4636 |
Teneligliptin hydrobromide
|
Teneligliptin (Teneligliptin hydrobromide anhydrous) 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. |
|
|
S5063 |
Trelagliptin succinate
|
Trelagliptin succinate (SYR472) is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM). |
|
|
E0122 |
Gemigliptin
|
Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.
|
|
|