HU 308 |
Katalog-Nr.GC13965
One-Click Copy Product Info
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CB2-receptor agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 256934-39-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment:[1,2] | |
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Cell lines |
Human liver sinusoidal endothelial cells (HLSECs); human coronary artery endothelial cells (HCAECs) |
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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. |
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Reaction Conditions |
HLSECs:0–4 μM for 4 h; HCSECs:3 μM for 4 h |
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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] | |
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Animal models |
C57Bl/6J mice |
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Dosage form |
HU-308 (10 mg/kg) was injected into the femoral vein right before the reocclusion. |
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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. |
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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. |
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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. |
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| Cas No. | 256934-39-1 | SDF | |
| Chemical Name | ((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 | ||
| Formula | C27H42O3 | M.Wt | 414.62 |
| Löslichkeit | A solution in methyl acetate | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4118 mL | 12.0592 mL | 24.1185 mL |
| 5 mM | 482.4 μL | 2.4118 mL | 4.8237 mL |
| 10 mM | 241.2 μL | 1.2059 mL | 2.4118 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solution in methyl acetate
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)