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    1. GPCR/G Protein
    2. 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 (13):

    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-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-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-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-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-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-P0231
    • 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-12584
      PF-5190457 Inhibitor
      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-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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