LY 338522: des-methyl metabolite of LY333531; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 10671412 |
| CHEMBL ID | 311543 |
| MeSH ID | M0450152 |
| Synonym |
|---|
| CHEMBL311543 , |
| 18-methylaminomethyl-(18s)-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8(13),9,11,22(27),23,25-nonaene-3,5-dione |
| bdbm50052034 |
| M2BQ56K56V , |
| ly 338522 |
| 191848-32-5 |
| n-desmethyl-ly 333531 |
| (9s)-6,7,10,11-tetrahydro-9-((methylamino)methyl)-9h,18h-5,21:12,17-dimethenodibenzo(e,k)pyrrolo(3,4-h)(1,4,13)oxadiazacyclohexadecine-18,20(19h)-dione |
| 9h,18h-5,21:12,17-dimethenodibenzo(e,k)pyrrolo(3,4-h)(1,4,13)oxadiazacyclohexadecine-18,20(19h)-dione, 6,7,10,11-tetrahydro-9-((methylamino)methyl)-, (9s)- |
| ly338522 |
| n-desmethyl ruboxistaurin |
| unii-m2bq56k56v |
| PD162009 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "No differences were observed in the pharmacokinetic parameters (area under the plasma concentration-time curve from time zero to infinity [AUC(infinity)], maximum plasma concentration [C(max)] and elimination half-life [t(1/2)]) of ruboxistaurin and metabolite 338522 between healthy and ESRD subjects Plasma concentrations of ruboxistaurin were below the lower limit of quantification by the time of haemodialysis." | ( Effects of chronic renal failure on the pharmacokinetics of ruboxistaurin and its active metabolite 338522. Chan, C; Lau, T; Poo, YK; Teng, L; Voelker, J; Wise, S; Yuen, E, 2006) | 0.33 |
| " Based on the pharmacokinetic and tolerability findings, no formal dosage adjustment of ruboxistaurin should be required for patients with any degree of renal impairment who are undergoing haemodialysis." | ( Effects of chronic renal failure on the pharmacokinetics of ruboxistaurin and its active metabolite 338522. Chan, C; Lau, T; Poo, YK; Teng, L; Voelker, J; Wise, S; Yuen, E, 2006) | 0.33 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Based on the pharmacokinetic and tolerability findings, no formal dosage adjustment of ruboxistaurin should be required for patients with any degree of renal impairment who are undergoing haemodialysis." | ( Effects of chronic renal failure on the pharmacokinetics of ruboxistaurin and its active metabolite 338522. Chan, C; Lau, T; Poo, YK; Teng, L; Voelker, J; Wise, S; Yuen, E, 2006) | 0.33 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Protein kinase C gamma type | Homo sapiens (human) | IC50 (µMol) | 0.2700 | 0.0001 | 1.0354 | 10.0000 | AID163880 |
| Protein kinase C alpha type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2193 | 1.0000 | AID164969 |
| Protein kinase C beta type | Homo sapiens (human) | IC50 (µMol) | 0.0050 | 0.0001 | 0.5542 | 10.0000 | AID163197; AID163341 |
| Protein kinase C delta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2585 | 1.0000 | AID164969 |
| Protein kinase C epsilon type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2585 | 1.0000 | AID164969 |
| Protein kinase C zeta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2585 | 1.0000 | AID164969 |
| Protein kinase C alpha type | Homo sapiens (human) | IC50 (µMol) | 0.2400 | 0.0001 | 0.9720 | 10.0000 | AID165309 |
| Protein kinase C eta type | Homo sapiens (human) | IC50 (µMol) | 0.0310 | 0.0001 | 0.7971 | 10.0000 | AID163855 |
| Protein kinase C gamma type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2640 | 1.1000 | AID164969 |
| Protein kinase C beta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2164 | 1.1000 | AID164969 |
| Protein kinase C epsilon type | Homo sapiens (human) | IC50 (µMol) | 1.1000 | 0.0001 | 0.8029 | 10.0000 | AID163687 |
| Protein kinase C zeta type | Homo sapiens (human) | IC50 (µMol) | 22.0000 | 0.0001 | 2.4453 | 10.0000 | AID164194 |
| Protein kinase C delta type | Homo sapiens (human) | IC50 (µMol) | 0.1700 | 0.0001 | 0.8448 | 10.0000 | AID163379 |
| Protein kinase C eta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2585 | 1.0000 | AID164969 |
| Protein kinase C theta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1600 | 0.0000 | 0.2585 | 1.0000 | AID164969 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (20.00) | 18.2507 |
| 2000's | 4 (80.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (12.74) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (40.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 3 (60.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||