HWL-088
目录号: PL10054 纯度: ≥98%
CAS No. :2378617-96-8
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中文名称
HWL-088
英文名称
HWL-088
英文别名
HWL-088;2-[2-fluoro-4-[[3-(2-methylphenyl)phenyl]methoxy]phenoxy]acetic acid;HWL088;GTPL10668;HWL 088;CID 139600331
Cas No.
2378617-96-8
分子式
C22H19FO4
分子量
366.38
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC 50 of 18.9 nM) with moderate PPARδ activity (EC 50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
性状
Solid
IC50 & Target[1][2]
PPARδ 570.9 nM (EC50) FFAR1/GPR40 18.9 nM
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 250 mg/mL (682.35 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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