Relamorelin

SKU: orb1985365

Description

Relamorelin is a potent, selective, and centrally permeable ghrelin receptor agonist (GHSR-1a, Ki = 0.42 nM). This pentapeptide analog elevates growth hormone secretion and accelerates gastric emptying, making it a valuable research tool for investigating conditions like gastroparesis and cachexia in both in vitro and in vivo studies.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	661472-41-9
MW	790.97
Purity	99.26%
Formula	C₄₃H₅₀N₈O₅S
SMILES	C([C@@H](NC([C@@H](CC=1C=2C(SC1)=CC=CC2)NC(=O)C3CCNCC3)=O)C(N[C@H](C(NC4(C(N)=O)CCNCC4)=O)CC5=CC=CC=C5)=O)C=6C=7C(NC6)=CC=CC7
Target	GHSR
Solubility	DMSO:50 mg/mL (63.21 mM)

Bioactivity

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Target IC50	native ghrelin:1.12 nM (Ki)\|native ghrelin:4.2 nM (EC50)\|GHS-R1a:0.42 nM (Ki)\|GHS-R1a:0.71 nM (EC50)
In Vivo	METHODS: C57BL6/J wt and GHR ko mice were treated with daily subcutaneous injections of rat ghrelin (5,000 nmol/kg) and RM-131 (50 or 500 nmol/kg), and the chronic effects of RM-131 on body weight, body composition (fat and lean mass), and food intake were measured. RESULTS Mice treated with 500 nmol/kg RM-131 showed a greater increase in food intake. Relamorelin(BIM28131, RM131) has a higher enzymatic stability in plasma than native ghrelin (half-life in rat plasma is 24 h vs. 1.9 h, respectively). hours), and when injected intravenously, its circulation half-life is prolonged 10-fold compared to native ghrelin. Read more...
In Vitro	Relamorelin (BIM28131, RM131) binds to the known ghrelin receptor (GHS-1a) with subnanomolar affinity (inhibition constant, 0.42 ± 0.063 nM), approximately three-fold higher than the affinity of native ghrelin (inhibition constant, 1.12 ± 0.17 nM); relamorelin (BIM28131, RM131) is six times more potent (EC50, 0.71 ± 0.09 nM) than native ghrelin (EC50, 4.2 ± 1.2 nM) in activating the GHS-1a receptor as assessed by in vitro calcium mobilization. Read more...

Storage & Handling

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Storage	store at low temperature,keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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BIM 28131, BIM 28163, BIM28131, BIM-28131, BIM28163, BIM-28163, hormone-releasing factor (GHRF), GHSR, Relamorelin, RM 131

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Compound Identifiers

PubChem CID

44251769 ↗

Key Properties

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No computed properties available.

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Relamorelin (orb1985365)

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Relamorelin

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Research Area

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Bioactivity

Storage & Handling

Alternative Names

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