| Identification | Back Directory | [Name]
HWL-088 | [CAS]
2378617-96-8 | [Synonyms]
HWL-088
2-(2-fluoro-4-((2'-methyl-[1,1'-biphenyl]-3-yl)methoxy)phenoxy)acetic acid | [Molecular Formula]
C22H19FO4 | [MDL Number]
MFCD32263430 | [MOL File]
2378617-96-8.mol | [Molecular Weight]
366.38 |
| Chemical Properties | Back Directory | [Boiling point ]
523.7±45.0 °C(Predicted) | [density ]
1.241±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (682.35 mM; Need ultrasonic) | [form ]
Solid | [pka]
3.14±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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]. | [in vivo]
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]. | Animal Model: | Male ob/ob mice[2] | | Dosage: | 40 mg/kg | | Administration: | Oral gavage; daily; for 30 days | | Result: | Improved β-cell function by up-regulation of pancreas duodenum homeobox-1, reduced fat accumulation in adipose tissue and alleviated fatty liver in ob/ob mice. |
| [IC 50]
FFAR1/GPR40: 18.9 nM (EC50); PPARδ: 570.9 nM (EC50) | [storage]
Store at -20°C | [References]
[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. |
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