1. Signaling Pathways
  2. GPCR/G Protein
  3. Free Fatty Acid Receptor

Free Fatty Acid Receptor (游离脂肪酸受体)

FFAR

游离脂肪酸受体 (FFAR) 是由游离脂肪酸 (FFA) 激活的 G 蛋白偶联受体 (GPCR)。四种特征明确的 FFAR 是 FFAR1/GPR40、FFAR2/GPR43、FFAR3/GPR41 和 FFAR4/GPR120。FFAR 根据激活每个 FFAR 的 FFA 配体的链长进行分类;FFA2 和 FFA3 由短链 FFA 激活,主要是乙酸盐、丁酸盐和丙酸盐。GPR84 由中链 FFA 激活,而 FFA1 和 GPR120 由中链或长链 FFA 激活。因此,每个 FFAR 都可以充当 FFA 传感器,对来自食物或食物衍生代谢物的特定 FFA 碳链长度具有选择性。据报道,FFAR 具有促进胰岛素和肠促胰岛素分泌、脂肪细胞分化、抗炎作用、神经元反应和味觉偏好等生理功能。FFAR 的这些生理功能可被认为是调节能量和免疫稳态。因此,FFAR 已成为治疗代谢紊乱(包括 2 型糖尿病和代谢综合征)的治疗策略的目标。

Free fatty acid receptors (FFARs) are G protein-coupled receptors (GPCRs) activated by free fatty acids (FFAs). The four well-characterized FFARs are FFAR1/GPR40, FFAR2/GPR43, FFAR3/GPR41, and FFAR4/GPR120. FFARs are categorized according to the chain length of FFA ligands that activate each FFAR; FFA2 and FFA3 are activated by short chain FFAs, mainly acetate, butyrate, and propionate. GPR84 is activated by medium-chain FFAs, whereas FFA1 and GPR120 are activated by medium- or long-chain FFAs. Thus, each FFAR can act as an FFA sensor with selectivity for a particular FFA carbon chain length derived from food or food derived metabolites. FFARs have been reported to have physiological functions such as facilitation of insulin and incretin hormone secretion, adipocyte differentiation, anti-inflammatory effects, neuronal responses, and taste preferences. These physiological functions of FFARs could be considered to regulate energy and immune homeostasis. Therefore, FFARs have been targeted in therapeutic strategies for the treatment of metabolic disorders including type 2 diabetes and metabolic syndrome.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-112603
    AP5 Agonist
    AP5 是一种有效的,具有口服活性,选择性 GPR40 受体激动剂,具有对内源性配体 (AgoPAM) 的正向变构调节作用。在大鼠和人肌醇一磷酸 (IP1) 实验中,AP5 作用于 GPR40 受体,EC50 值分别为 0.49 nM 和 0.8 nM。AP5 具有用于 II 型糖尿病研究的潜力。
    AP5
  • HY-111359
    GPR40 agonist 1 Agonist
    GPR40 agonist 1是有效,新颖的 GPR40 激动剂,对hGPR40 和 rGPR40的EC50 分别为 2 nM 和 17 nM。
    GPR40 agonist 1
  • HY-U00395
    GPR40 Agonist 2 Agonist
    GPR40 Agonist 2 是 GPR40 激动剂,可用于糖尿病的研究。
    GPR40 Agonist 2
目录号 产品名 / 同用名 应用 反应物种