Relamorelin TFA  (Synonyms: RM-131 TFA; BIM-28131 TFA)

产品描述：

Relamorelin(RM-131) TFA，一种生长素类似物，是一种选择性的生长素释放肽/生长激素促分泌素受体(GHSR)激动剂，对 GHS-1a 受体的 Ki 值为0.42nM。RelamorelinTFA是一种五肽，具有中枢渗透性。Relamorelin TFA增加生长激素水平，加速胃排空，具有用于恶病质、胃轻瘫和胃/肠运动障碍研究的潜力。

体外研究：

Relamorelin (RM-131) TFA shows ∼3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=1.12 nM). Relamorelin TFA is 6 times more potent (EC50=0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC50=4.2 nM) as assessed in vitro by calcium mobilization

体内研究：

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。

分子量：905.00
分子式：C45H51F3N8O7S
CAS 号：2863659-22-5