1. GPCR/G Protein
  2. Orexin Receptor (OX Receptor)

Orexin Receptor (OX Receptor)

Orexin receptors (OX receptor) include orexin 1 receptor and orexin 2 receptor. Orexin receptor type 1 (Ox1R or OX1), is a protein that in humans is encoded by the HCRTR1gene. The orexin 1 receptor (OX1), is a G-protein coupled receptor expressed in the hypothalamus and involved in the regulation of feeding behaviour. OX1 selectively binds the orexin-A neuropeptide. It shares 64% identity with OX2. The OX2 receptors, also known as hypocretin receptor 2, are located primarily in the cerebral cortex, paraventricular hypothalamus, nucleus accumbens, subthalamic and paraventricular thalamus where they are thought to regulate sleep-wakefulness. The OX2 receptor displays equal affinity for Orexin A and Orexin B. The human OX2 receptor gene has been localized to chromosome 6.

Orexin Receptor (OX Receptor) 相关产品 (20):

Cat. No. Product Name Effect Purity
  • HY-10895A
    SB-334867 free base Antagonist 99.77%
    SB-334867游离碱是非肽类食欲肽OX1受体拮抗剂,pKb为7.2。
  • HY-19320
    Orexin 2 Receptor Agonist Agonist 99.72%
    Orexin 2 Receptor Agonist是有效的选择性OX2R激动剂, EC50为23 nM。
  • HY-10805A
    Almorexant hydrochloride Antagonist 99.88%
    Almorexant(ACT078573)盐酸盐是OX1和OX2受体拮抗剂,Ki分别为1.3和0.17 nM。
  • HY-16725
    Lemborexant Antagonist 99.71%
    Lemborexant (E-2006)是食欲素受体OX1和OX2双重抑制剂,临床2期由于治疗失眠。
  • HY-100452
    TCS-OX2-29 Antagonist 99.18%
    TCS-OX2-29是一个强的和选择性的OX2受体拮抗剂,IC50是40 nM。
  • HY-10898
    SB-674042 Antagonist 99.70%
    SB-674042是非肽类食欲肽OX1受体拮抗剂,Kd为3.76 nM,比对OX2受体的抑制性高100倍。
  • HY-15653
    Filorexant Antagonist 98.95%
    Filorexant (MK-6096) 是食欲素受体OX1和OX2双重抑制剂,Ki 值小于3nM。
  • HY-19914
    MK-1064 Antagonist 99.15%
    MK-1064是一个选择性的2-SORA拮抗剂,可用于失眠患者的研究。
  • HY-13796
    IPSU Antagonist >98.0%
    IPSU是一种选择性,有口服活性和脑渗透性的OX2R拮抗剂,pKi值为7.85。
  • HY-101534
    GSK1059865 Antagonist 99.91%
    GSK1059865是有效地食欲素1受体 (orexin 1 receptor) 拮抗剂。
  • HY-70068
    SB-408124 Antagonist 98.27%
    SB408124是非肽类OX1受体拮抗剂,在全细胞和细胞膜分析中Ki为57 nM和27 nM,比对OX2受体的抑制性高50倍。
  • HY-10805
    Almorexant Antagonist 99.17%
    Almorexant(ACT078573)是OX1和OX2受体拮抗剂,Ki分别为1.3和0.17 nM。
  • HY-10806
    SB-649868 Antagonist 99.88%
    SB-649868 是一种口服有效的选择性食欲素 OX1OX 2 受体拮抗剂 (作用于 OX1 和 OX2 受体,pKi 分别为 9.4 和 9.5)。
  • HY-109095
    Nemorexant Antagonist 99.47%
    Nemorexant (ACT-541468) 是一种 orexin 受体拮抗剂,详细信息请参考专利文献 WO2015083094A1 中的化合物 example 7。作用于 Ox1Ox2 受体,IC50 分别为 2 nM 和 3 nM。
  • HY-P1349
    Orexin B, rat, mouse Agonist
    Orexin B, rat, mouse 是 Orexin 受体的内源性激动剂,与 OX1 和 OX2 结合的 Ki 值分别为420和36 nM。
  • HY-10900
    TCS 1102 Antagonist 99.77%
    TCS 1102是食欲肽OX受体拮抗剂,对OX2和OX1受体的Ki分别为0.2和3 nM。
  • HY-12301
    MK-3697 Antagonist 99.19%
    MK-3697是OX2受体的高效选择性拮抗剂,Ki值为0.95nM。
  • HY-10895
    SB-334867 Antagonist
    SB-334867是非肽类食欲肽OX1受体拮抗剂,pKb为7.2。
  • HY-76612
    SB-408124 Hydrochloride Antagonist 98.14%
    SB408124盐酸盐是非肽类OX1受体拮抗剂,在全细胞和细胞膜测试中Ki分别为57 nM和27 nM,比对OX2受体的抑制性高50倍。
  • HY-P1339
    Orexin B, human Agonist
    Orexin B, human是 Orexin 受体的内源性激动剂,与OX1和OX2结合的 Ki 值分别为 420 和 36 nM。
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