HWL-088 是一种高效的，具有口服活性的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂 (EC50 为 18.9 nM)，并具有中等 PPARδ 活性 (EC50 为 570.9 nM)。HWL-088 改善葡萄糖和脂质代谢，并具有抗糖尿病作用。
货号:ajcx34846
CAS:2378617-96-8
分子式:C22H19FO4
分子量：366.38
溶解度:DMSO : 250 mg/mL (682.35 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects[1][2].

HWL-088 (0.3 μM and 3μM) significantly increases insulin secretion fromMIN6 cells at 25 mM but not at 2 mM glucose. HWL-088 reveales a dose-dependent insulinotropic effect in the presence of 25-mM glucose[2].

HWL-088 (40 mg/kg; oral gavage; daily; for 30 days; ob/ob mice) treatment improves β-cell function by up-regulation of pancreas duodenum homeobox-1, reduces fat accumulation in adipose tissue and alleviated fatty liver in ob/ob mice. The effect of HWL-088 involves a reduction in hepatic lipogenesis and oxidative stress, increased lipoprotein lipolysis, glucose uptake, mitochondrial function and fatty acid β-oxidation[2].

[1]. Li Z, et al. Discovery of HWL-088: A highly potent FFA1/GPR40 agonist bearing a phenoxyacetic acid scaffold. Bioorg Chem. 2019 Nov;92:103209.
[2]. Yueming Chen, et al. HWL-088, a new potent free fatty acid receptor 1 (FFAR1) agonist, improves glucolipid metabolism and acts additively with metformin in ob/ob diabetic mice. Br J Pharmacol. 2020 May;177(10):2286-2302.