1. GPCR/G Protein
  2. 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 (16):

Cat. No. Product Name Effect Purity
  • HY-14734A
    Anamorelin hydrochloride Agonist 99.80%
    Anamorelin(RC1291; ONO-7643)是口服活性的饥饿素受体(ghrelin receptor)激动剂。
  • HY-14734
    Anamorelin Agonist 99.91%
    Anamorelin 是一种新型 ghrelin receptor 激动剂,FLIPR 检测中,EC50 为 0.74 nM。
  • HY-50844
    Ibutamoren Mesylate Agonist
    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-P0166
    Alexamorelin Inhibitor 98.93%
    Alexamorelin 是一种合成七肽,为 GHS 的抑制剂。
  • HY-P0169A
    GHRP-2 metabolite 1 Agonist 99.96%
    GHRP-2 metabolite 1是GHRP-2的代谢产物。生长激素释放肽-2(GHRP-2)是一种具有六个氨基酸单位的肽段(D-Ala-D-beta-+Nal-Ala-Trp-D-Phe-Lys-NH2)。GHRP-2是生长素释放肽的合成激动剂,GHRP-2可以显着促进生长激素的释放,改善动物和人类的血液生长激素浓度。
  • HY-12584
    PF-5190457 Agonist
    PF-5190457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-U00433A
    JMV 2959 hydrochloride Antagonist
    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-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-19235
    Examorelin Activator 99.79%
    Examorelin 是一种合成的生长激素释放肽,结合到生长激素促分泌素受体 (GHSR) 1a和非GHSR受体CD36,具有心脏保护作用。
  • HY-111343
    ONC212 Agonist 99.20%
    ONC212 是一种氟化的 ONC201 类似物,是一种有前景的抗癌药物,也是 GPR132 的选择性激动剂。
  • HY-103007
    TC-G-1008 Agonist 99.71%
    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-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-15243
    Capromorelin Tartrate Agonist 98.01%
    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-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-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-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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