1. Signaling Pathways
  2. GPCR/G Protein
  3. Mas-related G-protein-coupled Receptor (MRGPR)

Mas-related G-protein-coupled Receptor (MRGPR) 

Mas-related G-protein-coupled Receptor (MRGPR) is a novel family of sensory nerve specific orphan G protein coupled receptors (GPCRs). This family was characterized more than 30 years ago with the description of the Mas gene encoding for oncogene-like MAS receptors. The MRGPR family that now gathers more than 50 members in rodents and humans. On the basis of sequence homology, the family of MRGPRs can be divided into several subfamilies, namely, MRGPRA to MRGPRG and MRGPRX. Of these, the subfamilies MRGPR-A, MRGPR-B, and MRGPR-C are uniquely conserved in rodents, whereas the subfamily MRGPRX is characteristic among primates and humans. In humans, 4 MRGPRX genes, MRGPRX1, MRGPRX2, MRGPRX3, and MRGPRX4, have been described.

MRGPRs were first identified on specialized sensory neurons that encode itch (pruriceptors) and pain (nociceptors). Importantly, activation of Mrgprs expressed at the surface of sensory neurons has been shown to induce both itch and pain sensations. Most MRGPRs are associated with nociception and itch transmission, through their binding to various itch-inducing or painassociated substances: such as β–alanine, chloroquine (CQ), or substance P (SP).

Mas-related G-protein-coupled Receptor (MRGPR) 相关产品 (28):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-145195
    MrgprX2 antagonist-5
    MrgprX2 antagonist-5 是一种 MrgprX2 的拮抗剂。MrgprX2 antagonist-5 可用于皮肤炎症性疾病的研究。详细信息请参考专利文献 WO2020223255A1 中的化合物 16。
    MrgprX2 antagonist-5
  • HY-P3843
    Neuropeptide AF (cattle) Agonist
    Neuropeptide AF (cattle) 是一种酰胺化的十八肽,是 RFamide 神经肽。Neuropeptide AF (cattle) 充当 Mas 相关基因受体 A4 (MrgprA4) (Mas-related G-protein-coupled Receptor (MRGPR)) (EC50 约为 60 nM) 和 MrgprC11 (EC50 约为 300 nM) 的配体。Neuropeptide AF (cattle) 也激活 G 蛋白偶联受体 NPFF1 (Neuropeptide Y Receptor) (EC50 约为 25-325 nM) 和 NPFF2 (EC50 约为 1-5 nM)。Neuropeptide AF (cattle) 显示出抗阿片和相关的疼痛调节作用。
    Neuropeptide AF (cattle)
  • HY-143879
    MRGPRX1 agonist 3 Agonist
    MRGPRX1 agonist 3 (compound 1f) 是一种有效的 Mas 相关 G 蛋白偶联受体 X1 (MRGPRX1) 正向变构调节剂,EC50 为 0.22 μM。MRGPRX1 agonist 3 可用于神经性疼痛的研究。
    MRGPRX1 agonist 3
  • HY-147106
    Mrgx2 antagonist-1 Antagonist
    Mrgx2 antagonist-1 (实施例 1) 是一种有效的 Mrgx2 (Mas-related Gene X2) 拮抗剂。Mrgx2 antagonist-1 可用于 Mrgx2 介导的疾病和紊乱的研究。
    Mrgx2 antagonist-1
  • HY-148492
    Mrgx2 antagonist-2 Antagonist
    Mrgx2 antagonist-2 是一种 Mrgx2 拮抗剂 (参考专利中的 Example 123),pIC50 为 8.6。Mrgx2 antagonist-2 可用于 MrgX2 介导的疾病研究。
    Mrgx2 antagonist-2
  • HY-143878
    MRGPRX1 agonist 2 Agonist
    MRGPRX1 agonist 2 (compound 1a) 是一种有效的 Mas 相关 G 蛋白偶联受体 X1 (MRGPRX1) 正向变构调节剂,EC50 为 0.48 μM。MRGPRX1 agonist 2 可用于神经性疼痛研究。
    MRGPRX1 agonist 2
  • HY-P1241A
    BAM(8-22) TFA
    BAM(8-22) TFA 是前脑啡肽 A 的蛋白水解切割产物,是 Mas 相关的 G 蛋白偶联受体 (Mrgprs),MrgprC11 和 hMrgprX1 的有效激活剂,并以 Mrgpr 依赖性方式诱导小鼠抓挠。
    BAM(8-22) TFA
  • HY-145193A
    (R)-MrgprX2 antagonist-3 Antagonist
    (R)-MrgprX2 antagonist-3 是一种 MrgprX2 的拮抗剂。MrgprX2 antagonist-3 可用于皮肤炎症性疾病的研究。详细信息请参考专利文献 WO2021092240A1 中的化合物 E118。
    (R)-MrgprX2 antagonist-3