Relamorelin TFA (Synonyms: RM-131 TFA; BIM-28131 TFA)
產品描述：
Relamorelin(RM-131) TFA，一種生長素類似物，是一種選擇性的生長素釋放肽/生長激素促分泌素受體(GHSR)激動劑，對 GHS-1a 受體的 Ki 值為0.42nM。RelamorelinTFA是一種五肽，具有中樞滲透性。Relamorelin TFA增加生長激素水平，加速胃排空，具有用于惡病質、胃輕癱和胃/腸運動障礙研究的潛力。
體外研究：
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
體內研究：
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 號：2863659-22-5
