trelagliptin: a dipeptidyl peptidase IV inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 15983988 |
| CHEMBL ID | 1650443 |
| CHEBI ID | 134715 |
| SCHEMBL ID | 175726 |
| MeSH ID | M000602678 |
| Synonym |
|---|
| 2-[6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethyl]-4-fluorobenzonitrile |
| bdbm50335784 |
| CHEBI:134715 |
| trelagliptin |
| syr-472 |
| CHEMBL1650443 , |
| D10178 |
| 865759-25-7 |
| trelagliptin (usan) |
| benzonitrile, 2-((6-((3r)-3-amino-1-piperidinyl)-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)- pyrimidinyl)methyl)-4-fluoro- |
| q836owg55h , |
| unii-q836owg55h |
| 2-((6-((3r)-3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)- yl)methyl)-4-fluorobenzonitrile |
| trelagliptin [usan:inn] |
| HY-15408 |
| CS-1041 |
| trelagliptin [usan] |
| 2-({6-[(3r)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl}methyl)-4-fluorobenzonitrile |
| trelagliptin [who-dd] |
| benzonitrile, 2-((6-((3r)-3-amino-1-piperidinyl)-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)-pyrimidinyl)methyl)-4-fluoro- |
| trelagliptin [inn] |
| trelagliptin [mi] |
| S7513 , |
| SCHEMBL175726 |
| DTXSID00235678 |
| (r)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl)methyl)-4-fluorobenzonitrile |
| AC-30279 |
| AKOS026674097 |
| EX-A470 |
| trelagliptin(syr472) |
| mfcd22572746 |
| 2-[[6-[(3r)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile |
| AS-75009 |
| 2-({6-[(3r)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl}methyl)-4-fluorobenzonitrile |
| trelagliptin(syr-472) |
| 6RL , |
| 2-[[6-[(3~{r})-3-azanylpiperidin-1-yl]-3-methyl-2,4-bis(oxidanylidene)pyrimidin-1-yl]methyl]-4-fluoranyl-benzenecarboni |
| (r)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl)methyl)-4-fluorobenzonitrile. |
| 865759-25-7 (free base) |
| DB15323 |
| CCG-268122 |
| NCGC00378845-01 |
| Q27287099 |
| A855303 |
| nsc-802901 |
| nsc802901 |
| 2-[[6-[(3~{r})-3-azanylpiperidin-1-yl]-3-methyl-2,4-bis(oxidanylidene)pyrimidin-1-yl]methyl]-4-fluoranyl-benzenecarboni trile |
Trelagliptin is a once-weekly taking selective dipeptidyl peptidase-4 (DPP-4) inhibitor and a long-term effective hypoglycemic medicine. Its effects for the treatment of diabetes-related cognitive impairment have only sometimes been explored.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Trelagliptin could lower the mRNA expression of inflammatory factors such IL-1β, TNF-α, and IL-6 in DM rats." | ( Trelagliptin relieved cognitive impairment of diabetes mellitus rats: Involvement of PI3K/Akt/GSK-3β and inflammation pathway. Chen, Q; Guo, X; Lei, M; Liu, C; Liu, X; Ouyang, C; Ren, Z; Shu, T; Yang, X; Yao, Y, 2023) | 3.07 |
Treatment with trelagliptin exhibited an improvement in insulin resistance. Trelagliptin treatment showed no significant changes in FMD (2.42 ± 2.7% at baseline vs. .
| Excerpt | Reference | Relevance |
|---|---|---|
| "Trelagliptin treatment showed no significant changes in FMD (2.42 ± 2.7% at baseline vs." | ( Effect of trelagliptin on vascular endothelial functions and serum adiponectin level in patients with type 2 diabetes: a preliminary single-arm prospective pilot study. Betou, K; Fujiwara, R; Ida, S; Imataka, K; Ishihara, Y; Kaneko, R; Kobayashi, C; Monguchi, K; Murata, K; Takahashi, H; Uchida, A, 2016) | 1.56 |
| "Treatment with trelagliptin exhibited an improvement in insulin resistance." | ( The protective effects of trelagliptin on high-fat diet-induced nonalcoholic fatty liver disease in mice. Jin, X; Wang, G; Wang, H; Wang, K; Wu, B; Xu, W; Zhang, B; Zhang, L, 2021) | 1.26 |
This study aims to develop and validate a simple, rapid and sensitive ultra-performance liquid chromatography with tandem mass spectrometry (UHPLC-MS/MS) method for exploring pharmacokinetic characteristics of trelagliptin.
| Excerpt | Reference | Relevance |
|---|---|---|
| "This study aims to develop and validate a simple, rapid and sensitive ultra-performance liquid chromatography with tandem mass spectrometry (UHPLC-MS/MS) method for exploring pharmacokinetic characteristics of trelagliptin." | ( A rapid and sensitive UHPLC-MS/MS assay for the determination of trelagliptin in rat plasma and its application to a pharmacokinetic study. Cai, JP; Chen, Z; Hu, GX; Hu, XX; Lan, T; Tang, PF; Yang, CC; Yuan, LJ, 2016) | 0.86 |
| "This study aimed to build a mathematical model of physiologically based pharmacokinetic combined DPP-4 occupancy (PBPK-DO) in humans to provide some recommendations for dosing adjustment in patients with renal impairment." | ( Prediction of pharmacokinetics and pharmacodynamics of trelagliptin and omarigliptin in healthy humans and in patients with renal impairment using physiologically based pharmacokinetic combined DPP-4 occupancy modeling. Li, B; Liu, H; Liu, Y; Ren, C; Wang, G; Wu, C; Yu, S; Zhang, J, 2022) | 0.97 |
This study investigated the effects of trelagliptin and remogliflozin, alone and in combination with alpha lipoic acid (ALA), on cardiac biomarkers in diabetic cardiomyopathy.
| Excerpt | Reference | Relevance |
|---|---|---|
| "A total of 680 patients received the following antidiabetic therapies: trelagliptin monotherapy (n = 248), combination with a sulfonylurea (n = 158), a glinide (n = 67), an α-glucosidase inhibitor (n = 65), a biguanide (n = 70), or a thiazolidinedione (n = 72)." | ( Long-term safety and efficacy of a novel once-weekly oral trelagliptin as monotherapy or in combination with an existing oral antidiabetic drug in patients with type 2 diabetes mellitus: A 52-week open-label, phase 3 study. Inagaki, N; Kaku, K; Kuroda, S; Sano, H; Seki, Y, 2016) | 0.91 |
| "This study investigated the effects of trelagliptin and remogliflozin, alone and in combination with alpha lipoic acid (ALA), on cardiac biomarkers in diabetic cardiomyopathy (DCM)." | ( Impacts of trelagliptin and remogliflozin alone and in combination with Alpha Lipoic Acid on cardiac function in streptozotocin-induced diabetes mellitus in rats. Abdullah Ali, M; Kareem Hamad, B; Naji Alhassani, A, 2023) | 1.57 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The absolute bioavailability of (R)-trelagliptin was identified to be 128." | ( The Chiral Bioconversion and Pharmacokinetic Analysis of Trelagliptin in Beagle Dog Plasma by LC-MS/MS. Sun, L; Xi, W; Yu, J; Zhang, H; Zhou, L; Zou, Q, 2019) | 1.03 |
Trelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor, shows sustained efficacy by once-weekly dosing in type 2 diabetes patients.
| Class | Description |
|---|---|
| benzenes | Any benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives. |
| nitrile | A compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 1.7740 | 10.0000 | AID566681 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 1.7536 | 10.0000 | AID566685 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.0151 | 10.0000 | AID566684 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.8005 | 10.0000 | AID566682 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | IC50 (µMol) | 0.0022 | 0.0001 | 0.4444 | 10.0000 | AID1444855; AID1493016; AID566627 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | Ki | 0.0051 | 0.0000 | 0.3414 | 2.2000 | AID1493022 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.3983 | 10.0000 | AID566683 |
| Dipeptidyl peptidase 8 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0019 | 2.6532 | 10.0000 | AID566628 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1638380 | Anti-diabetic activity in db/db mouse assessed as increase in glucose tolerance at 10 mg/kg, po dosed once weekly for 8 weeks by OGTT | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1444855 | Inhibition of human recombinant DPP4 using Gly-Pro-7-amido-4-methyl-coumarin as substrate incubated for 15 mins by fluorescence assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Synthetic Approaches to the New Drugs Approved During 2015. |
| AID1493031 | Tmax in Sprague-Dawley rat at 25 mg/kg, po or 5 mg/kg, iv administered as single dose by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493026 | Metabolic stability in mouse liver microsomes assessed as parent compound remaining at 1 mM incubated for 5 mins measured up to 60 mins by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493028 | Half life in rat liver microsomes at 1 mM by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1395907 | Elimination half life in human | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID566684 | Inhibition of CYP2D6 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493043 | In vivo inhibition of DPP4 activity in ICR mouse plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566630 | Half life in human liver microsomes by LC/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493030 | Half life in Sprague-Dawley rat at 25 mg/kg, po administered as single dose by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493027 | Metabolic stability in monkey liver microsomes assessed as parent compound remaining at 1 mM incubated for 5 mins measured up to 60 mins by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493035 | Oral bioavailability in Sprague-Dawley rat at 25 mg/kg administered as single dose by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493022 | Competitive inhibition of human DPP4 using Gly-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 5 to 10 mins by Line-weaver-Burk plot analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566688 | Toxicity in dog by GLP toxicology study | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493041 | In vivo inhibition of DPP4 activity in ICR mouse plasma at 3 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566687 | Toxicity in rat by GLP toxicology study | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1638382 | Anti-diabetic activity in db/db mouse assessed as increase in glucose-induced insulin secretion at 10 mg/kg, po dosed once weekly for 8 weeks pretreated for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT r | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1638383 | Anti-diabetic activity in db/db mouse assessed as HbA1c levels at 10 mg/kg, po dosed once weekly for 8 weeks | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1651642 | Inhibition of human DPP4 assessed as dissociation half life using Gly-Pro-p-nitroaniline as substrate | 2020 | Journal of natural products, 03-27, Volume: 83, Issue:3 | Natural Products as Sources of New Drugs over the Nearly Four Decades from 01/1981 to 09/2019. |
| AID1638379 | Anti-diabetic activity in db/db mouse assessed as reduction in fasting blood glucose at 10 mg/kg, po dosed once weekly for 8 weeks | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1493042 | In vivo inhibition of DPP4 activity in ICR mouse plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured over 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1638370 | Anti-diabetic activity in 6 h-fasted db/db mouse assessed as inhibition of DPP4 in plasma at 10 mg/kg, po administered as single dose pretreated for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID566628 | Inhibition of human DPP8 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID566681 | Inhibition of CYP1A2 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493032 | AUC (0 to t) in Sprague-Dawley rat at 25 mg/kg, po administered as single dose by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493039 | In vivo inhibition of DPP4 activity in Sprague-Dawley rat plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1444856 | Inhibition of human recombinant DPP4 using Gly-Pro-p-nitroaniline as substrate assessed as dissociation half life preincubated for 70 mins followed by 50 fold dilution in buffer containing substrate measured every 10 secs by fluorescence assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Synthetic Approaches to the New Drugs Approved During 2015. |
| AID1493024 | Metabolic stability in dog liver microsomes assessed as parent compound remaining at 1 mM incubated for 5 mins measured up to 60 mins by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1638373 | Anti-diabetic activity in 8 hrs-fasted ICR mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po pretre at ed for 60 mins followed by glucose challenge and measured after 120 mins post glucose challenge by OGTT rel at ive to con | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
| AID1493038 | In vivo inhibition of DPP4 activity in Sprague-Dawley rat plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured over 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493016 | Inhibition of human DPP4 using Gly-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 5 to 10 mins | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493025 | Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 mM incubated for 5 mins measured up to 60 mins by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566678 | Antidiabetic activity in Zucker fa/fa rat assessed as increase in glucose tolerance at 1 and 0.3 mg/kg, po | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493034 | Apparent volume of distribution during terminal phase in Sprague-Dawley rat at 25 mg/kg, po or 5 mg/kg, iv administered as single dose by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566679 | Antidiabetic activity in Zucker fa/fa rat assessed as increase in postprandial plasma insulin level at 1 and 0.3 mg/kg, po | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493040 | In vivo inhibition of DPP4 activity in ICR mouse plasma at 3 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured over 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566683 | Inhibition of CYP2C19 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493029 | Half life in human liver microsomes at 1 mM by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566686 | Inhibition of human ERG up to 30 uM | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID566629 | Half life in rat liver microsomes by LC/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493037 | In vivo inhibition of DPP4 activity in Sprague-Dawley rat plasma at 3 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566685 | Inhibition of CYP3A4 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID566682 | Inhibition of CYP2C9 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| AID1493023 | Metabolic stability in rat liver microsomes assessed as parent compound remaining at 1 mM incubated for 5 mins measured up to 60 mins by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493033 | Clearance in Sprague-Dawley rat at 25 mg/kg, po or 5 mg/kg, iv administered as single dose by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID1493036 | In vivo inhibition of DPP4 activity in Sprague-Dawley rat plasma at 3 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured over 52 hrs by fluorescence asay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
| AID566627 | Inhibition of human DPP4 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 28 (66.67) | 24.3611 |
| 2020's | 14 (33.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (49.24) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 10 (23.81%) | 5.53% |
| Reviews | 7 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 25 (59.52%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||