1. Signaling Pathways
  2. GPCR/G Protein
  3. Succinate Receptor 1

Succinate Receptor 1 (琥珀酸受体)

SUCNR1; GPR91

琥珀酸受体(SUCNR1,也称为 GPR91)是一种 G 蛋白偶联受体,与 P2Y 嘌呤受体家族密切相关。琥珀酸受体被确定为由生理水平的克雷布斯循环中间体琥珀酸和其他二羧酸(如马来酸)激活。它在多种组织中表达,包括血细胞、脂肪组织、肝脏、视网膜和肾脏。在这些组织中,这种受体及其配体琥珀酸最近成为局部应激情况下的新介质,包括缺血、缺氧、毒性和高血糖。除其他外,琥珀酸受体参与将免疫细胞募集到移植组织。此外,它被证明在糖尿病视网膜病变的发展中起着关键作用。然而,最突出的是,肾脏局部增加的琥珀酸水平和琥珀酸受体活化,刺激全身和局部肾素-血管紧张素系统的作用开始显现:琥珀酸受体是高血压发展和糖尿病和代谢综合征中可能的纤维化的关键介质。

The succinate receptor (SUCNR1, also known as GPR91) is a G protein-coupled receptor that is closely related to the family of P2Y purinoreceptors. The Succinate receptor was identified as being activated by physiological levels of the Kreb's cycle intermediate succinate and other dicarboxylic acids such as maleate. It is expressed in a variety of tissues, including blood cells, adipose tissue, the liver, retina, and kidney. In these tissues, this receptor and its ligand succinate have recently emerged as novel mediators in local stress situations, including ischemia, hypoxia, toxicity, and hyperglycemia. Amongst others, the succinate receptor is involved in recruitment of immune cells to transplanted tissues. Moreover, it was shown to play a key role in the development of diabetic retinopathy. However, most prominently, the role of locally increased succinate levels and succinate receptor activation in the kidney, stimulating the systemic and local renin–angiotensin system, starts to unfold: the succinate receptor is a key mediator in the development of hypertension and possibly fibrosis in diabetes mellitus and metabolic syndrome.

Succinate Receptor 1 相关产品 (6):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-130246
    NF-56-EJ40 99.92%
    NF-56-EJ40 是一种有效,高亲和力和高度选择性的人 SUCNR1 (GPR91) 拮抗剂,IC50 为 25 nM,Ki 为 33.5 nM,对大鼠 SUCNR1 几乎没有活性。 NF-56-EJ40 对人源化大鼠 SUCNR1 具有高亲和力,Ki 值为 17.4 nM。
    NF-56-EJ40
  • HY-125791
    cis-Epoxysuccinic acid Agonist 99.00%
    cis-Epoxysuccinic acid 是 succinate receptor (SUCNR1/GPR91) 的激动剂。cis-Epoxysuccinic acid 抑制 cAMP 的水平,其 EC50 值为 2.7 µM。cis-Epoxysuccinic acid 可用于心血管系统的研究。
    cis-Epoxysuccinic acid
  • HY-154946
    SUCNR1-IN-1 Inhibitor 99.33%
    SUCNR1-IN-1 (Compound 20) 是一种 SUCNR1 抑制剂 (IC50: 对 hSUCNR1 为 88 nM)。SUCNR1-IN-1 可用于类风湿关节炎、肝纤维化或肥胖的研究。
    SUCNR1-IN-1
  • HY-126217
    hGPR91 antagonist 1 98.71%
    hGPR91 Antagonist 1 (Compound 4c) 是一种有效的 GPR91 拮抗剂,对于人 GPR91 的 IC50 为 7 nM。
    hGPR91 antagonist 1
  • HY-145919
    hGPR91 antagonist 3 98.82%
    hGPR91 Antagonist 3 (Compound 5g) 是一种有效的具有口服活性的 GPR91 拮抗剂,对于人 GPR91 和大鼠 GPR91 的 IC50 分别为 35 nM 和 135 nM。
    hGPR91 antagonist 3
  • HY-130246A
    NF-56-EJ40 hydrochloride
    NF-56-EJ40 hydrochloride 是一种有效,高亲和力和高度选择性的人 SUCNR1 (GPR91) 拮抗剂,IC50 为 25 nM,Ki 为 33.5 nM,对大鼠 SUCNR1 几乎没有活性。 NF-56-EJ40 hydrochloride 对人源化大鼠 SUCNR1 具有高亲和力,Ki 值为 17.4 nM。
    NF-56-EJ40 hydrochloride