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O-304

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Chemical Structure| 1261289-04-6 同义名 : O-304X
CAS号 : 1261289-04-6
货号 : A1176833
分子式 : C16H11Cl2N3O2S
纯度 : 99%+
分子量 : 380.248
MDL号 : MFCD31657425
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 30 mg/mL(78.9 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 AMPK activated protein kinase (AMPK), a master regulator of energy homeostasis, is activated in response to an energy shortage. When pathological conditions cause ATP levels to fall, AMPK is activated to restore cellular energy homeostasis[1]. O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. It exhibits a great potential as a drug to treat type 2 diabetes (T2D) and associated cardiovascular complications. Mice fed with a high-fat diet (HFD), denoted DIO mice, were treated by oral gavage with vehicle, O304, Metformin, or O304+Metformin (100 mg/kg/day) each for 8 weeks. O304 and O304+Metformin, but not Metformin, averted the HFD-provoked increase in fasted glucose and plasma insulin levels and inhibited insulin resistance[2]. Postoperative pain mice models made by incision in the left plantar hindpaw were treated by oral gavage with vehicle, metformin 200 mg/kg, O304 200 mg/kg and O304 200 mg/kg plus metformin 200 mg/kg, for 3 days. O304 or metformin increased von Frey thresholds (reduced mechanical hypersensitivity) in plantar incision mice compared to vehicle-treated incision mice[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.15mL

2.63mL

1.31mL

26.30mL

5.26mL

2.63mL

参考文献

[1]Steinberg GR, Carling D. AMP-activated protein kinase: the current landscape for drug development. Nat Rev Drug Discov. 2019 Jul;18(7):527-551. doi: 10.1038/s41573-019-0019-2. PMID: 30867601.

[2]Steneberg P, Lindahl E, Dahl U, Lidh E, Straseviciene J, Backlund F, Kjellkvist E, Berggren E, Lundberg I, Bergqvist I, Ericsson M, Eriksson B, Linde K, Westman J, Edlund T, Edlund H. PAN-AMPK activator O304 improves glucose homeostasis and microvascular perfusion in mice and type 2 diabetes patients. JCI Insight. 2018 Jun 21;3(12):e99114. doi: 10.1172/jci.insight.99114. PMID: 29925691; PMCID: PMC6124394.

[3]Das V, Kroin JS, Moric M, McCarthy RJ, Buvanendran A. Antihyperalgesia effect of AMP-activated protein kinase (AMPK) activators in a mouse model of postoperative pain. Reg Anesth Pain Med. 2019 Jun 21:rapm-2019-100651. doi: 10.1136/rapm-2019-100651. Epub ahead of print. PMID: 31229963.