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HU 308 目录号 GC13965

CB2-receptor agonist

规格 价格 库存 购买数量
1mg
¥377.00
现货
5mg
¥1,599.00
现货
10mg
¥2,834.00
现货
25mg
¥6,123.00
现货

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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Cell experiment:[1,2]

Cell lines

Human liver sinusoidal endothelial cells (HLSECs); human coronary artery endothelial cells (HCAECs)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

HLSECs:0–4 μM for 4 h; HCSECs:3 μM for 4 h

Applications

In HCSECs or HLSECs, HU-308 treatment reduced the expression of both ICAM-1 and VCAM-1, which was induced by TNFα. HU-308 attenuated TNFα treatment induced RhoA activation (4.0-fold vs. control) and NF-B Activation. HU-308 inhibited TNFα-induced monocyte adhesion in aortas.

Animal experiment:[2]

Animal models

C57Bl/6J mice

Dosage form

HU-308 (10 mg/kg) was injected into the femoral vein right before the reocclusion.

Applications

Pretreatment of mice with HU-308 decreases the I/R-induced tissue damage, inflammatory cell infiltration, tissue and serum TNF-α, MIP-1, and MIP-2 levels, tissue lipid peroxidation and apoptosis.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Rajesh M, Mukhopadhyay P, Bátkai S, et al. CB2-receptor stimulation attenuates TNF-alpha-induced human endothelial cell activation, transendothelial migration of monocytes, and monocyte-endothelial adhesion. Am J Physiol Heart Circ Physiol. 2007 Oct;293(4):H2210-8.

[2]. Rajesh M, Pan H, Mukhopadhyay P, et al. Cannabinoid-2 receptor agonist HU-308 protects against hepatic ischemia/reperfusion injury by attenuating oxidative stress, inflammatory response, and apoptosis. J Leukoc Biol. 2007 Dec;82(6):1382-9.

Chemical Properties

Cas No. 256934-39-1 SDF
别名 N/A
化学名 ((1S,4S,5S)-4-(2,6-dimethoxy-4-(2-methyloctan-2-yl)phenyl)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methanol
Canonical SMILES OCC1=C[C@H](C(C(OC)=CC(C(C)(C)CCCCCC)=C2)=C2OC)[C@H]3C(C)(C)[C@@H]1C3
分子式 C27H42O3 分子量 414.62
溶解度 A solution in methyl acetate 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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产品描述

HU-308 is a selective agonist of CB2-receptor with a Ki value of 20 nM. The Ki value for CB1-receptor is >10 µM.
Cannabinoid 2 receptor (CB2-receptor) belongs to the seven transmembranes G protein-coupled receptor superfamily. It is mainly distributed in peripheral tissue associated with immune functions.
In HLSECs, HU-308 markedly reduced the expression of both ICAM-1 and VCAM-1, which was induced by TNFα. HU-308 attenuated TNF- treatment induced RhoA activation (4.0-fold vs. control) and NF-B Activation. HU-308 inhibited TNFα-induced monocyte adhesion in aortas ex vivo [1].
HU-308 increased both primary neurosphere generation and neural progenitor self-renewal. HU-308 increased the number of BrdU incorporating cells in a CB2-dependent manner. HU-308 stimulated ERK and Akt [2].
Pretreatment of mice with HU-308 decreases the I/R-induced tissue damage, inflammatory cell infiltration,tissue and serum TNF-α, MIP-1, and MIP-2 levels, tissue lipid peroxidation and apoptosis [3].

References:
[1].Rajesh M, Mukhopadhyay P, Bátkai S, et al. CB2-receptor stimulation attenuates TNF-alpha-induced human endothelial cell activation, transendothelial migration of monocytes, and monocyte-endothelial adhesion. Am J Physiol Heart Circ Physiol. 2007 Oct;293(4):H2210-8.
[2].Palazuelos J, Aguado T, Egia A, et al. Non-psychoactive CB2 cannabinoid agonists stimulate neural progenitor proliferation. FASEB J. 2006 Nov;20(13):2405-7.
[3].Rajesh M, Pan H, Mukhopadhyay P, et al. Cannabinoid-2 receptor agonist HU-308 protects against hepatic ischemia/reperfusion injury by attenuating oxidative stress, inflammatory response, and apoptosis. J Leukoc Biol. 2007 Dec;82(6):1382-9.