| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
Relamorelin, formerly known as BIM28131 and RM131, is a centrally penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) potentially useful for the treatment of diabetic gastroparesis, chronic idiopathic constipation, and anorexia nervosa. It is a pentapeptide and analogue of ghrelin with improved potency and pharmacokinetics. In humans, relamorelin produces increases in plasma growth hormone, prolactin, and cortisol levels, and, like other GHSR agonists, increases appetite.
| Targets |
Growth hormone secretagogue receptor (GHSR, also referred to as the ghrelin receptor; GHR), specifically the GHSR1a spliced variant. It has high in vitro affinity to bind and activate GHSR1a [2].
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| ln Vitro |
Compared to native ghrelin (Ki=1.12 nM), relamorelin (RM-131) exhibits an affinity for GHS-1a that is almost three times stronger (Ki=0.42 nM). Relamorelin is six times more effective than native ghrelin (EC50=4.2 nM) at activating GHS-1a receptors, according to an assessment of in vitro calcium mobilization [1].
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| ln Vivo |
Relamorelin (RM-131; subcutaneous injection; 50–500 nmol/kg/day; continuous infusion for 5 days) decreases fat mass loss and body weight. Rats given relamorelin (500 nmol/kg/day; continuous infusion for 5 days) eat more and gain more weight [1]. A single subcutaneous injection of RM-131 (250–500 nmol/kg) increases acute food intake in wt mice, but not in growth hormone secretagogue receptor (GHR) ko mice [2].
In wildtype (wt) mice, a single subcutaneous injection of RM-131 at 250 or 500 nmol/kg induces an immediate, dose-dependent increase in acute food intake, with the peak effect observed 2 hours post-injection. The 500 nmol/kg dose of RM-131 shows a significantly greater increase in food intake (area under the curve, p < 0.001) compared to an equimolar dose (500 nmol/kg) of native ghrelin [2]. In wt mice, chronic systemic administration of RM-131 (50 or 500 nmol/kg) via daily subcutaneous injections for seven days significantly promotes body weight gain (both p < 0.01 vs. vehicle) and increases adiposity (body fat mass). The body weight gain is dose-dependent, with the 500 nmol/kg dose being significantly more effective than the 50 nmol/kg dose (p < 0.0001) and a 10-fold higher dose (5,000 nmol/kg) of native ghrelin (p < 0.05). The increase in body weight is attributed to an increase in body fat, not lean tissue mass. Cumulative food intake is significantly increased only in the wt mice treated with the higher dose of 500 nmol/kg RM-131 (p < 0.05) [2]. In mice lacking the ghrelin receptor (GHR ko), RM-131 (at 250 and 500 nmol/kg for acute, and 50 and 500 nmol/kg for chronic studies) has no effect on acute food intake, body wei |
| Enzyme Assay |
The primary evidence for its target engagement is derived from in vivo experiments using GHR knockout mice, which show a complete loss of RM-131's anabolic effects, thereby confirming its specificity for the ghrelin receptor in a physiological context [2].
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| Animal Protocol |
Animal/Disease Models: F344/NTacfBR male rats with tumor implantation [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:Caused food intake Increased volume (tumor/saline 41.4 g, tumor/BIM-28131 72.5 g) and weight gain (tumor/saline -10.3%, tumor/BIM-28131 +19.5%). Acute Food Intake Study: Male C57BL/6J wildtype (wt) and GHR knockout (ko) mice (10-week-old, N=8 per group) were single-housed and received a single subcutaneous injection. Test compounds were dissolved in H₂O containing 5% mannitol. Treatment groups included vehicle control (H₂O with 5% mannitol), rat ghrelin (500 or 5,000 nmol/kg), or RM-131 (250 or 500 nmol/kg). Food intake was measured at 0.5, 1, 2, 4, 8, 12, and 24 hours post-injection [2]. Chronic Treatment Study: Male C57BL/6J wt and GHR ko mice (13-week-old, N=8 per group) were double-housed and treated for seven consecutive days with once-daily subcutaneous injections. Test compounds were dissolved in H₂O containing 5% mannitol. Treatment groups included vehicle control (H₂O with 5% mannitol), rat ghrelin (5,000 nmol/kg), or RM-131 (50 or 500 nmol/kg). Body composition (fat and lean tissue mass) was assessed on day 7 using MRI technology [2]. Acute Food Intake Study: Male C57BL/6J wildtype (wt) and GHR knockout (ko) mice (10-week-old, N=8 per group) were single-housed and received a single subcutaneous injection. Test compounds were dissolved in H₂O containing 5% mannitol. Treatment groups included vehicle control (H₂O with 5% mannitol), rat ghrelin (500 or 5,000 nmol/kg), or RM-131 (250 or 500 nmol/kg). Food intake was measured at 0.5, 1, 2, 4, 8, 12, and 24 hours post-injection [2]. Chronic Treatment Study: Male C57BL/6J wt and GHR ko mice (13-week-old, N=8 per group) were double-housed and treated for seven consecutive days with once-daily subcutaneous injections. Test compounds were dissolved in H₂O containing 5% mannitol. Treatment groups included vehicle control (H₂O with 5% mannitol), rat ghrelin (5,000 nmol/kg), or RM-131 (50 or 500 nmol/kg). Body composition (fat and lean tissue mass) was assessed on day 7 using MRI technology [2]. |
| ADME/Pharmacokinetics |
As a pentapeptide, RM-131 confers increased bioavailability and improved pharmacokinetic properties compared to native ghrelin, which has a relatively short half-life (varying from 30 minutes in rats to 240 minutes in humans). Compared to native human ghrelin, RM-131 is approximately 10- to 100-fold more potent, and it is 600- to 1,800-fold more potent compared to other ghrelin mimetics tested in clinical trials [2].
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| Toxicity/Toxicokinetics |
Human Studies - Adverse Effects: In a phase IIB study (NCT02357420) involving patients with diabetic gastroparesis who received twice-daily subcutaneous injections of relamorelin (10, 30, or 100 µg), adverse effects were noted. Relamorelin was responsible for worsening glycemic control in 14.5% of patients in a dose-dependent manner, necessitating insulin or other diabetic drug dosage modifications for some patients [3].
Safety studies of relamorelin have not reported any electrocardiogram (ECG) changes, such as QTc prolongation, which is a concern with other available drugs like metoclopramide, domperidone, and cisapride [3]. |
| References |
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| Additional Infomation |
Relamorelin has been investigated for therapeutic and basic scientific research purposes, including for gastroparesis, gastric motility disorders, diabetes, Parkinson's disease, and chronic constipation.
Drug Indications Treatment of Gastroparesis RM-131 is a pentapeptide ghrelin analog developed to overcome the pharmacological limitations of native ghrelin, particularly its short half-life. The therapeutic potential of RM-131 is being explored for conditions like cachexia, sarcopenia, myopenia, gastroparesis, and anorexia nervosa. At the time of this publication, RM-131 was in phase 2 clinical trials for the treatment of diabetic gastroparesis and intestinal dysmotility disorders. Preliminary clinical studies reported that a single subcutaneous administration of RM-131 accelerates gastric emptying in type 2 diabetic patients with gastroparesis [2]. |
| Molecular Formula |
C43H50N8O5S
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|---|---|
| Exact Mass |
790.362
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| CAS # |
661472-41-9
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| Related CAS # |
Relamorelin TFA;2863659-22-5;Relamorelin acetate;1809080-14-5
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| PubChem CID |
85364156
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
1216.2±65.0 °C at 760 mmHg
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| Flash Point |
689.3±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.692
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| LogP |
5.22
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
57
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| Complexity |
1410
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| Defined Atom Stereocenter Count |
3
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| SMILES |
S1C2C=CC=CC=2C(=C1)C[C@H](C(N[C@H](CC1=CNC2C=CC=CC1=2)C(N[C@@H](CC1C=CC=CC=1)C(NC1(C(N)=O)CCNCC1)=O)=O)=O)NC(C1CNCCC1)=O
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| InChi Key |
IPMQOGDSJZQLFX-BIBZJUPHSA-N
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| InChi Code |
InChI=1S/C43H50N8O5S/c44-42(56)43(16-19-45-20-17-43)51-41(55)34(21-27-9-2-1-3-10-27)49-39(53)35(22-29-25-47-33-14-6-4-12-31(29)33)50-40(54)36(48-38(52)28-11-8-18-46-24-28)23-30-26-57-37-15-7-5-13-32(30)37/h1-7,9-10,12-15,25-26,28,34-36,45-47H,8,11,16-24H2,(H2,44,56)(H,48,52)(H,49,53)(H,50,54)(H,51,55)/t28?,34-,35+,36+/m0/s1
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| Chemical Name |
N-((R)-3-(benzo[b]thiophen-3-yl)-1-(((R)-1-(((S)-1-((4-carbamoylpiperidin-4-yl)amino)-1-oxo-3-phenylpropan-2-yl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-1-oxopropan-2-yl)piperidine-3-carboxamide
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| Synonyms |
BIM28131 BIM 28131 BIM-28131 BIM-28163 BIM 28163 BIM28163 RM131 RM-131 RM 131 Relamorelin
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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