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CAS No.: 1261289-04-6

O-304 Catalog No. CSN24788

Synonyms: O-304X

O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a drug to treat type 2 diabetes (T2D) and associated cardiovascular complications [1][2].

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400-920-2911

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实验方案

技术信息

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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6299 mL
- 13.1493 mL
- 26.2986 mL
- 5 mM
- 0.5260 mL
- 2.6299 mL
- 5.2597 mL
- 10 mM
- 0.2630 mL
- 1.3149 mL
- 2.6299 mL

技术信息

CAS号

1261289-04-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H11Cl2N3O2S

运输

蓝冰

分子量

380.25

别名

O-304X

溶解度

DMSO	19.5 mg/mL (51.3 mM)
Water	insoluble

动物实验配方

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