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Ulimorelin

Cat. No. M30676
Ulimorelin Structure
Synonym:

TZP-101

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Quality Control & Documentation
Biological Activity

Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.

Chemical Information
Molecular Weight 538.65
Formula C30H39FN4O4
CAS Number 842131-33-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Joyce James, et al. Neurogastroenterol Motil. The effects of ulimorelin, a ghrelin agonist, on liquid gastric emptying and colonic transit in humans

[2] John Broad, et al. Eur J Pharmacol. Analysis of the ghrelin receptor-independent vascular actions of ulimorelin

[3] R V Pustovit, et al. Neurogastroenterol Motil. The mechanism of enhanced defecation caused by the ghrelin receptor agonist, ulimorelin

[4] Monica Shaw, et al. Dis Colon Rectum. Safety and efficacy of ulimorelin administered postoperatively to accelerate recovery of gastrointestinal motility following partial bowel resection: results of two randomized, placebo-controlled phase 3 trials

[5] Grant Bochicchio, et al. World J Surg. Ghrelin agonist TZP-101/ulimorelin accelerates gastrointestinal recovery independently of opioid use and surgery type: covariate analysis of phase 2 data

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Keywords: Ulimorelin, TZP-101 supplier, Ghrelin Receptor/GHSR, inhibitors, activators


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