O-7460
目录号 : KCM11713 CAS No. : 1572051-31-0 纯度 : ≥95%
In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; ) by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (ICs > 10 µM) and does not bind to CB or CB cannabinoid receptors (Ks > 10 µM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-dependently inhibit high-fat diet intake and reduce body weight.
规格 价格 是否有货 数量
500μg
In-stock
1mg
In-stock
5mg
In-stock

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生物活性

O-7460 is a potent and selective DAGLα inhibitor, with an IC50 of 0.69 μM. O-7460 shows selectivity over onoacylglycerol lipase (MAGL), human CB1 and CB2 cannabinoid receptors. O-7460 can decrease HFD-caused an up-regulation of 2-AG levels.

体外研究

O-7460 (10 μM; 20 min) decreases the Ionomycin (3 μM)-induced formation of 2-AG in N18TG2 cells.

体内研究

O-7460 (6-12 mg/kg; a single i.p.) induces a time- and dose-dependent decrease in high-fat diet (HFD) intake and counteracts the body weight increase of mice.
O-7460 (12 mg/kg; i.p.) decreases the HFD-caused an up-regulation of 2-AG levels in the hypothalamus and liver of mice.

 

Animal Model: Seven-week-old male C57BL/6N inbred mice were administrated high-fat diet (HFD) diet
Dosage: 6, 12 mg/kg
Administration: A single i.p.
Result: Induced a time (30 min, 60 min and 14 h after O-7460 administration) and dose-dependent decrease in HFD intake.
The highest dose significantly counteracted the body weight increase.
 
分子式
C25H48FO5P
分子量
478.62
CAS号
1572051-31-0
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
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