O-7460 - CAS:1572051-31-0

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O-7460

目录号 : KCM11713 CAS No. : 1572051-31-0 纯度 : ≥95%

Data Sheet 产品使用指南

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.

IC₅₀&Target

DAGLα

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

纯度： ≥95%

Data Sheet

产品使用指南

Bisogno T, et, al. A novel fluorophosphonate inhibitor of the biosynthesis of the endocannabinoid 2-arachidonoylglycerol with potential anti-obesity effects. Br J Pharmacol. 2013 Jun;169(4):784-93.

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