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

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 (18):

Cat. No. Product Name Effect Purity
  • 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-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-14734
    Anamorelin Agonist 99.91%
    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)
    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-13964A
    YIL781 hydrochloride Antagonist
    YIL781 hydrochloride 是有效的、具有口服活性的胃促生长素受体 (GHSR) 的拮抗剂。YIL781 hydrochloride 可改善大鼠体内葡萄糖稳态。YIL781 hydrochloride 可抑制饥饿素诱导的钙反应,pIC50 值分别为 7.90 和 8.27。
  • 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-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-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-P0231
    AZP-531
    AZP-531是一种用于提高血糖控制并减轻体重的非格酸化生长素释放肽类似物。
  • 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-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-P1432
    K-(D-1-Nal)-FwLL-NH2 Antagonist
    K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • 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。
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA Antagonist
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-14734B
    Anamorelin Fumarate Agonist
    Anamorelin(RC1291; ONO-7643)延胡索酸盐是口服活性的饥饿素受体激动剂。
  • HY-U00433
    JMV 2959 Antagonist
    JMV 2959 是一种生长激素促分泌素受体 1a 型 (GHS-R1a) 拮抗剂,其 IC50 值为 32 nM。
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