| 名称 | Relamorelin |
| 描述 | Relamorelin(BIM28131, RM131) is a selective and potent ghrelin/growth hormone secretagogue receptor (GHSR) agonist with high affinity for GHS-1a receptor (Ki value is 0.42 ± 0.063 nM). Relamorelin(BIM28131, RM131) is also a centrally permeable pentapeptide analog that can increase growth hormone levels and accelerate gastric emptying, and has the potential to study cachexia. |
| 体外活性 | 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. [2] |
| 体内活性 | 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. [1]
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.[2] |
| 存储条件 | 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. |
| 溶解度 | DMSO : 50 mg/mL (63.2 mM), Sonication is recommended.
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| 关键字 | Relamorelin |
| 相关产品 | Ibutamoren Mesylate | Capromorelin Tartrate | AnaMorelin hydrochloride | YIL 781 | Anamorelin | CJC-1295 acetate(863288-34-0 free base) | L-692429 | NF-56-EJ40 hydrochloride | TM-N1324 | Cortistatin-8 acetate |
| 相关库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 已知活性化合物库 | GPCR靶点分子库 |
United States
