Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D0W9VW
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| Former ID |
DCL000255
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| Drug Name |
TZP-101
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| Synonyms |
Ulimorelin; TZP-101; TZP 101; UNII-LGI67MCW2S; 842131-33-3; LGI67MCW2S; CHEMBL1923502; Ulimorelin [USAN:INN]; Ulimorelin (USAN/INN); SCHEMBL804500; TZP101; GTPL3535; CHEMBL1963249; DTXSID00233139; BDBM50359256; DB12128; D09981; (3R,6S,9R,12R)-6-cyclopropyl-12-[(4-fluorophenyl)methyl]-3,8,9-trimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione; D-Phenylalanine, (2S)-N-((2R)-2-(2-(3-aminopropyl)phenoxy)propyl)-2- cyclopropylglycyl-N-methyl-D-alanyl-4-fluoro-, (3-1)-lactam
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| Drug Type |
Small molecular drug
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| Indication | Gastrointestinal disease [ICD-11: DE2Z] | Phase 2b | [1], [2] | |
| Gastroparesis [ICD-11: DA41.00] | Phase 2b | [1], [2] | ||
| Ileus [ICD-11: DA93.0; ICD-10: K56.0] | Phase 2b | [1], [2] | ||
| Company |
Tranzyme
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| Structure |
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Download2D MOL |
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| Formula |
C30H39FN4O4
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| Canonical SMILES |
CC1CNC(C(=O)N(C(C(=O)NC(C(=O)NCCCC2=CC=CC=C2O1)CC3=CC=C(C=C3)F)C)C)C4CC4
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| InChI |
1S/C30H39FN4O4/c1-19-18-33-27(23-12-13-23)30(38)35(3)20(2)28(36)34-25(17-21-10-14-24(31)15-11-21)29(37)32-16-6-8-22-7-4-5-9-26(22)39-19/h4-5,7,9-11,14-15,19-20,23,25,27,33H,6,8,12-13,16-18H2,1-3H3,(H,32,37)(H,34,36)/t19-,20-,25-,27+/m1/s1
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| InChIKey |
WGYPAJVJMXQXTR-ABNZCKJZSA-N
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| CAS Number |
CAS 842131-33-3
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| PubChem Compound ID | ||||
| PubChem Substance ID | ||||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Growth hormone secretagogue receptor 1 (GHSR) | Target Info | Agonist | [3], [4], [5] |
| KEGG Pathway | cAMP signaling pathway | |||
| Neuroactive ligand-receptor interaction | ||||
| NetPath Pathway | Leptin Signaling Pathway | |||
| Reactome | Peptide ligand-binding receptors | |||
| G alpha (q) signalling events | ||||
| WikiPathways | GPCRs, Class A Rhodopsin-like | |||
| Gastrin-CREB signalling pathway via PKC and MAPK | ||||
| Peptide GPCRs | ||||
| GPCR ligand binding | ||||
| GPCR downstream signaling | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3535). | |||
| REF 2 | Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26. | |||
| REF 3 | Contribution of protein binding to the pharmacokinetics of the ghrelin receptor agonist TZP-101 in healthy volunteers and adults with symptomatic gastroparesis: two randomized, double-blind studies and a binding profile study. Clin Drug Investig. 2009;29(6):409-18. | |||
| REF 4 | Ghrelin receptor agonist (TZP-101) accelerates gastric emptying in adults with diabetes and symptomatic gastroparesis. Aliment Pharmacol Ther. 2009 Jun 1;29(11):1179-87. | |||
| REF 5 | Effect of the ghrelin receptor agonist TZP-101 on colonic transit in a rat model of postoperative ileus. Eur J Pharmacol. 2009 Feb 14;604(1-3):132-7. | |||
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