1. Signaling Pathways
  2. GPCR/G Protein
  3. GHSR


GHSR (Growth hormone secretagogue receptor) is a member of the G-protein coupled receptor family. GHSR may play a role in energy homeostasis and regulation of body weight. The pathway activated by binding of ghrelin to the growth hormone secretagogue receptor, GHSR1a, regulates the activation of the downstream mitogen-activated protein kinase, Akt, nitric oxide synthase, and AMPK cascades in different cellular systems. One of the important features of GHSR1a displays constitutive activity possessing basal activity in the absence of an agonist, resulting in a high degree of receptor internalization as well as of signaling activity. Inverse agonists for the ghrelin receptor could be particularly interesting for the treatment of obesity. A range of selective ligands for the GHSR receptor are now available and are being developed for several clinical applications. GHSR agonists have appetite-stimulating and growth hormone-releasing effects, and are likely to be useful for the treatment of muscle wasting and frailty associated with old-age and degenerative diseases. On the other hand, GHSR antagonists have anorectic effects and are likely to be useful for the treatment of obesity.

GHSR 相关产品 (15):

Cat. No. Product Name Effect Purity
  • HY-50844
    Ibutamoren Mesylate Agonist 98.42%
    Ibutamoren Mesylate 是一种有效的,非肽段类生长激素促分泌素受体 (GHSR) 激动剂。
  • HY-14734A
    Anamorelin hydrochloride Agonist 99.92%
    Anamorelin(RC1291; ONO-7643)是口服活性的饥饿素受体(ghrelin receptor)激动剂。
  • HY-14734
    Anamorelin Agonist 99.62%
    Anamorelin 是一种新型 ghrelin receptor 激动剂,FLIPR 检测中,EC50 为 0.74 nM。
  • HY-U00433A
    JMV 2959 hydrochloride Antagonist 98.02%
    JMV 2959 hydrochloride 是一种生长激素促分泌素受体 1a 型 (GHS-R1a) 拮抗剂,作用于 LLC-PK1 细胞,抑制 GHS-R1aIC50 值为 32±3 nM。
  • HY-103007
    TC-G-1008 Agonist 99.03%
    TC-G-1008 (GPR39-C3) 是有效的,有口服活性的 GPR39 激动剂,对大鼠和人类受体的EC50值分别为0.4 和 0.8 nM。
  • HY-P1306
    Obestatin(rat) 是一种由 Ghrelin 基因编码的肽,由 23 个氨基酸组成。Obestatin(rat) 抑制食物摄入,抑制空肠收缩,并减少体重增加。Obestatin(rat) 是 G 蛋白偶联受体 39 (GPR39) 的内源性配体,具有抗炎,抗心肌梗塞和抗氧化的作用。
  • HY-P1306A
    Obestatin(rat) TFA
    Obestatin(rat) TFA 是一种由 Ghrelin 基因编码的肽,由 23 个氨基酸组成。Obestatin(rat) TFA 抑制食物摄入,抑制空肠收缩,并减少体重增加。Obestatin(rat) TFA 是 G 蛋白偶联受体 39 (GPR39) 的内源性配体,具有抗炎,抗心肌梗塞和抗氧化的作用。
  • HY-50760
    L-692585 Agonist
    L-692585 是一种有效的非肽基生长激素促分泌素受体 (GHS-R1a) 激动剂,Ki 值为 0.8 nM。L-692585 可直接作用于生长激素,诱导 GH 释放。
  • HY-108699
    TM-N1324 Agonist 98.91%
    TM-N1324 是 G 蛋白偶联受体 39 (GPR39) 的激动剂,在 Zn2+ 存在的情况下,对人和鼠 GPR39EC50 值分别为 9 nM 和 5 nM,在 Zn2+ 不存在的情况下,对人和鼠 GPR39EC50 值分别为 280 nM 和 180 nM。
  • HY-15243
    Capromorelin Tartrate Agonist 98.19%
    Capromorelin Tartrate 是一种可口服的,有效的growth hormone secretagogue receptor (GHSR)激动剂,对hGHS-R1a的Ki值为 7 nM。
  • HY-P0231
  • HY-12584
    PF-5190457 Inhibitor 98.05%
    PF-5190457 (PF-05190457) 是一种有效,选择性的生长素释放肽受体 (ghrelin receptor) 反向激动剂, pKi 值为 8.36。
  • HY-P0166A
    Alexamorelin Met 1 Inhibitor 99.82%
    Alexamorelin Met 1 是alexamorelin的代谢产物。七肽Ala-His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2(Alexamorelin)是在体外试验中抑制生长激素促分泌素结合的合成分子。
  • HY-10957
    L-692429 Agonist
    L-692429 (MK-0751) 是一种苯并内酰胺的衍生物,也是一种非肽基生长激素促分泌素 (GHS) 激动剂。L-692429 以 Ki 值为 63 nM 来结合 G 蛋白偶联受体 (G protein-coupled receptor)。
  • HY-14903
    Ulimorelin Agonist
    Ulimorelin (TZP-101) 是生长素释放肽受体 (GRLN) 激动剂,EC50 为 29 nM,Ki 为 16 nM。Ulimorelin 是一种促运动剂,通过竞争性拮抗 α1-肾上腺素受体引起血管舒张。Ulimorelin 可以刺激肠蠕动,可用于营养不良。
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