Relamorelin TFA - ≥99% , CAS No.2863659-22-5

CAS: 2863659-22-5 Cat. No.: R648040 Peso molecular: 905.00

GRADE & PURITY ≥99%

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K i of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research

In Vitro

Relamorelin (RM-131) TFA shows ∼3 times greater affinity for GHS-1a (K i =0.42 nM) than native ghrelin (K i =1.12 nM). Relamorelin TFA is 6 times more potent (EC 50 =0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC 50 =4.2 nM) as assessed in vitro by calcium mobilization. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Relamorelin (RM-131; 50-500 nmol/kg/day; s.c.; continuous infusion for 5 days) TFA decreases the loss of body mass and fat mass. Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) TFA increases the food intake and weight gain in rats . RM-131 (250-500 nmol/kg; a single s.c.) TFA stimulates acute food intake in wt but not growth hormone secretagogue receptor (GHR) ko mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: F344/NTacfBR male rats implanted with tumor Dosage: 50, 500 nmol/kg/day Administration: SC; continuous infusion at a rate of 0.5 μL/h for 5 d Result: 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%).

Form:Solid

IC50& Target:Ki: 0.42 nM (GHS-1a)

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K i of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone

Condiciones de almacenamiento de almacenamiento

Desiccated, Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Pureza

≥99%

Nombres e identificadores

• Peso molecular: 905.00

Propiedades químicas y físicas

• Solubilidad: H2O : 100 mg/mL (110.50 mM; Need ultrasonic)