| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Ki: 0.42 nM (GHS-1a)[1]
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|---|---|
| ln Vitro |
The affinity of relamorelin (RM-131) TFA for GHS-1a is almost three times higher than that of native ghrelin (Ki=1.12 nM; Ki=0.42 nM). In vitro calcium mobilization testing revealed that relamorelin TFA is six times more effective (EC50=0.71 nM) than native ghrelin (EC50=4.2 nM) at activating the GHS -1a receptor[1].
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| ln Vivo |
Body mass and fat mass loss are lessened by relamorelin (RM-131; 50–500 nmol/kg/day; sc; continuous infusion for 5 days) TFA. Rats given relamorelin (500 nmol/kg/day; continuous infusion for 5 days) TFA eat more and gain more weight[1]. A single SC dose of RM-131 (250–500 nmol/kg) TFA increases acute food intake in wt mice, but not in GHR-KO mice.
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| Animal Protocol |
Animal/Disease Models: F344/NTacfBR male rats implanted with tumor[1]
Doses: 50, 500 nmol/kg/day Route of Administration: SC; continuous infusion at a rate of 0.5 μL/h for 5 d Experimental Results: Resulted in an increase in food intake (tumor/saline 41.4 g, tumor/BIM-28131 72.5 g) and weight gain (tumor/saline -10.3%, tumor/BIM-28131 +19.5%). |
| References |
[1]. DeBoer MD, et, al. Ghrelin treatment causes increased food intake and retention of lean body mass in a rat model of cancer cachexia. Endocrinology. 2007 Jun;148(6):3004-12.
[2]. Fischer K, et, al. The Pentapeptide RM-131 Promotes Food Intake and Adiposity in Wildtype Mice but Not in Mice Lacking the Ghrelin Receptor. Front Nutr. 2015 Jan 12;1:31. [3]. Zatorski H, et, al. Relamorelin and other ghrelin receptor agonists - future options for gastroparesis, functional dyspepsia and proton pump inhibitors-resistant non-erosive reflux disease. J Physiol Pharmacol. 2017 Dec;68(6):797-805. [4]. Matthew Heckroth, et al. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299. [5]. Victor Chedid, et al. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197. |
| Molecular Formula |
C45H51F3N8O7S
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|---|---|
| Molecular Weight |
905.00
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| CAS # |
2863659-22-5
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| Related CAS # |
Relamorelin;661472-41-9;Relamorelin acetate;1809080-14-5
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| SMILES |
C(C1=CNC2=CC=CC=C12)[C@H](C(=O)N[C@@H](CC1C=CC=CC=1)C(=O)NC1(CCNCC1)C(=O)N)NC(=O)[C@H](NC(C1CCNCC1)=O)CC1=CSC2=CC=CC=C12.C(F)(F)(F)C(=O)O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 100 mg/mL (110.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (55.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1050 mL | 5.5249 mL | 11.0497 mL | |
| 5 mM | 0.2210 mL | 1.1050 mL | 2.2099 mL | |
| 10 mM | 0.1105 mL | 0.5525 mL | 1.1050 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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