Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C30H39FN4O4.ClH |
| Molecular Weight | 575.114 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](CC3=CC=C(F)C=C3)C(=O)NCCCC4=C(O1)C=CC=C4
InChI
InChIKey=WZRLNIOAVAFOOD-UZAUECDSSA-N
InChI=1S/C30H39FN4O4.ClH/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);1H/t19-,20-,25-,27+;/m1./s1
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C30H39FN4O4 |
| Molecular Weight | 538.6535 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Ulimorelin (TZP101) is a small molecule, intravenously administered, ghrelin receptor agonist that is being developed by Lyric Pharmaceuticals. Ulimorelin stimulates intestinal motility, but also reduces blood pressure in rodents and humans and dilates blood vessels. It has been proposed as a treatment for intestinal motility disorders. Ulimorelin has progressed to phase III human clinical trials for the treatment of postoperative ileus.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Optimization of the potency and pharmacokinetic properties of a macrocyclic ghrelin receptor agonist (Part I): Development of ulimorelin (TZP-101) from hit to clinic. | 2011 Dec 22 |
|
| The mechanism of enhanced defecation caused by the ghrelin receptor agonist, ulimorelin. | 2014 Feb |
|
| Analysis of the ghrelin receptor-independent vascular actions of ulimorelin. | 2015 Apr 5 |
Sample Use Guides
Partial bowel resection: Thirty-minute intravenous infusions (160 ug/kg, 480 ug/kg ulimorelin, or placebo) once daily were started within 60 minutes after the end of surgery and ended at the first of the following: primary efficacy end point fulfilled (defined below), hospital discharge, or 7 days treatment.
Route of Administration:
Intravenous
Ulimorelin (0.03-30uM) inhibited phenylephrine-induced contractions of rat saphenous (IC50=0.6uM; Imax=66±5%; n=3-6) and mesenteric arteries (IC50=5uM, Imax=113±16%; n=3-4). In mesenteric arteries, ulimorelin, 1-10uM, caused a surmountable rightward shift in the response to phenylephrine (0.01-1000uM; pA2=5.7; n=3-4). Ulimorelin is an agonist of G-protein coupled receptor (Ki=16 nM, EC50=29 nM).
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 04:40:27 GMT 2023
by
admin
on
Sat Dec 16 04:40:27 GMT 2023
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| Record UNII |
0FU3439KDP
|
| Record Status |
Validated (UNII)
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| Record Version |
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874336-43-3
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0FU3439KDP
Created by
admin on Sat Dec 16 04:40:27 GMT 2023 , Edited by admin on Sat Dec 16 04:40:27 GMT 2023
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56925693
Created by
admin on Sat Dec 16 04:40:27 GMT 2023 , Edited by admin on Sat Dec 16 04:40:27 GMT 2023
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| Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS |
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ACTIVE MOIETY |
