ffa2-agonist 1

LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor. The RON receptor tyrosine kinase has been identified as an important mediator of KRAS oncogene addiction and is overexpressed in the majority of pancreatic cancers. Preclinical studies show that inhibition of RON function decreases pancreatic cancer cell migration, invasion, and survival and can sensitize pancreatic cancer cells to chemotherapy. RON receptor tyrosine kinase is a potential as a therapeutic target.

FFA2 agonist-1 (Compound 4) 是一种游离脂肪酸受体 2 (FFA2 GPR43) 的激动剂，EC50为81 nM。在 β-arrestin-2 募集试验中，其EC50为1.2 μM，而在cAMP抑制试验中表现出的EC50为0.53 μM。该化合物能够激发食欲调节肽 YY (PYY) 粘膜反应，对脂肪积聚、肠道功能和食物摄入有抑制作用，适用于肥胖研究。

TUG-499 是一种选择性游离脂肪酸受体 1 (FFAR1 或 GPR40)激动剂（EC50 ： 7.39）。TUG-499对 FFAR1 或 GPR40的亲和力超过相关受体 FFA2、FFA3 和核受体 PPARγ，以及其他不同的受体、离子通道和转运蛋白。TUG-499 可用于研究 2 型糖尿病。

LON63114, also known as FFA2-Agonist-1 is a selective orthosteric agonist of human FFA2. FFA2-Agonist-1 is potentially useful in the treatment of gastrointestinal disorders and inflammatory bowel diseases. LON63114 was reported in WO2011076732. This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https: www.medkoo.com page naming).

MOMBA是一种针对人类自由脂肪酸2(hFFA2)工程化受体和设计药物激活的设计受体(DREADD)的选择性正交激动剂，对野生型hFFA2、hFFA3和小鼠FFA2无活性。MOMBA能够在表达hFFA2-DREADD受体的细胞中抑制forskolin刺激的cAMP水平，其功效改善且与山梨酸的效力相当。在hFFA2-DREADD转基因小鼠中，MOMBA治疗显著降低肠道传输速度，并促进依赖浓度的结肠隐窝GLP-1释放。该化合物具有口服生物利用度。