| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Ki: 0.42 nM (GHS-1a)[1]
Targets the ghrelin/growth hormone secretagogue receptor (GHSR-1a) with high affinity, exhibiting a Ki of 0.42 nM, which is nearly three times higher than that of native ghrelin (Ki = 1.12 nM). It is a selective agonist, mimicking the effects of the endogenous hormone ghrelin on appetite, growth hormone release, and gastrointestinal motility. |
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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].
In vitro, Relamorelin TFA potently activates GHSR-1a. Calcium mobilization assays reveal that Relamorelin is six times more effective than native ghrelin in activating the GHS-1a receptor, with an EC50 of 0.71 nM compared to ghrelin‘s EC50 of 4.2 nM. This superior potency is a key feature distinguishing it from the endogenous ligand. |
| 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.
In vivo, Relamorelin TFA effectively increases body weight and food intake in animal models. In rats, continuous subcutaneous infusion of 500 nmol/kg/day for five days resulted in increased food consumption and weight gain. It also lessened the loss of body mass and fat mass in a rat model of cancer cachexia, demonstrating its potential to counteract wasting syndromes. |
| Enzyme Assay |
No cell-free enzyme data is applicable, as Relamorelin targets a GPCR. Standard radioligand binding assays for GHSR-1a are performed using membranes from cells that overexpress the receptor. These are incubated with a radiolabeled ghrelin analog and various concentrations of Relamorelin to determine its binding affinity (Ki). These assays are cell-based but can be considered receptor binding studies.
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| Cell Assay |
Functional agonism is assessed in cells expressing the GHSR-1a receptor using calcium mobilization assays. Cells are loaded with a calcium-sensitive fluorescent dye, then treated with varying concentrations of Relamorelin. The resulting change in fluorescence is measured to calculate the agonist‘s potency (EC50) and efficacy. This confirms that the compound activates the receptor.
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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%). In the rat cancer cachexia model, F344/NTacfBR male rats are implanted with a tumor. Relamorelin is administered at doses of 50 and 500 nmol/kg/day via subcutaneous continuous infusion at a rate of 0.5 microL/h for 5 days. Key endpoints include measuring food intake and body weight daily. At the end of the study, body composition (fat and lean mass) is analyzed. |
| ADME/Pharmacokinetics |
Detailed PK data for Relamorelin is available from its clinical trials. As a pentapeptide, it has low oral bioavailability and is administered via subcutaneous injection. In humans, it has a relatively short half-life (approximately 1-2 hours) and is rapidly cleared. These properties make it suitable for acute administration to stimulate gastric emptying.
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| Toxicity/Toxicokinetics |
Relamorelin has been evaluated in Phase 2 and Phase 3 clinical trials for diabetic gastroparesis. No significant safety issues were reported in these trials; it was generally well-tolerated. The most common side effects were mild and included injection site reactions, headache, and diarrhea. Importantly, it was not associated with the significant increases in blood glucose seen with other ghrelin agonists.
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| References |
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| Additional Infomation |
Relamorelin is an investigational drug that has undergone clinical trials but has not yet received regulatory approval for any indication. It was previously under development by Allergan (now AbbVie) for diabetic gastroparesis. While it showed promise in early trials, a Phase 3 program was discontinued. It remains a potent and highly useful research tool for studying GHSR-1a biology.
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| Molecular Formula |
C45H51F3N8O7S
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|---|---|
| Molecular Weight |
904.996059656143
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| Exact Mass |
904.355
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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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| PubChem CID |
162641838
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
64
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| Complexity |
1480
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| Defined Atom Stereocenter Count |
3
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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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| InChi Key |
YKEWFQMJVBJGEJ-GTKQDQPASA-N
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| InChi Code |
InChI=1S/C43H50N8O5S.C2HF3O2/c44-42(56)43(16-20-46-21-17-43)51-41(55)34(22-27-8-2-1-3-9-27)49-39(53)35(23-29-25-47-33-12-6-4-10-31(29)33)50-40(54)36(48-38(52)28-14-18-45-19-15-28)24-30-26-57-37-13-7-5-11-32(30)37;3-2(4,5)1(6)7/h1-13,25-26,28,34-36,45-47H,14-24H2,(H2,44,56)(H,48,52)(H,49,53)(H,50,54)(H,51,55);(H,6,7)/t34-,35+,36+;/m0./s1
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| Chemical Name |
4-[[(2S)-2-[[(2R)-2-[[(2R)-3-(1-benzothiophen-3-yl)-2-(piperidine-4-carbonylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]piperidine-4-carboxamide;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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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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