HU 211 |
| Catalog No.GC13074 |
NMDA antagonist, novel and non-competitive
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 112924-45-5
Sample solution is provided at 25 µL, 10mM.
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HU 211 is a novel and non-competitive antagonist of NMDA [1].
N-Methyl-D-aspartate (NMDA) is an amino acid derivative that acts as a specific agonist at the NMDA receptor and only binds to and regulates the NMDA receptor.
HU 211 is a novel and non-competitive NMDA antagonist. In culture neurones, HU 211 inhibited NMDA-mediated neurotoxicity in a dose dependent way with EC50 value of 3.8 µM. Also, HU 211 inhibited [3H]MK-801 binding to rat forebrain membranes in a competitive way with Ki value of 11.0 µM [1]. In rat alveolar macrophage cell line and murine peritoneal macrophages, HU 211 inhibited nitric oxide and TNFα production induced by lipopolysaccharide (LPS) [4].
In a global ischemia gerbil model, HU-211 (4 mg/kg) significantly induced neuroprotection in the CA1 subfield of the hippocampus [2]. In the rat with closed head injury (CHI), HU-211 (5 mg/kg) significantly improved neurological severity score (NSS) and slightly reduced edema. In the Morris water maze, HU-211 significantly improved the abilities impaired by CHI [3]. In BALB/c mice injected with 10 mg/kg LPS, HU-211 reduced lethality to 9 and 67%. In Sprague-Dawley rats, HU-211 abolished the hypotensive response induced by LPS [4].
References:
[1]. Eshhar N, Striem S, Biegon A. HU-211, a non-psychotropic cannabinoid, rescues cortical neurones from excitatory amino acid toxicity in culture. Neuroreport, 1993, 5(3): 237-240.
[2]. Bar-Joseph A, Berkovitch Y, Adamchik J, et al. Neuroprotective activity of HU-211, a novel NMDA antagonist, in global ischemia in gerbils. Mol Chem Neuropathol, 1994, 23(2-3): 125-135.
[3]. Shohami E, Novikov M, Bass R. Long-term effect of HU-211, a novel non-competitive NMDA antagonist, on motor and memory functions after closed head injury in the rat. Brain Res, 1995, 674(1): 55-62.
[4]. Gallily R, Yamin A, Waksmann Y, et al. Protection against septic shock and suppression of tumor necrosis factor alpha and nitric oxide production by dexanabinol (HU-211), a nonpsychotropic cannabinoid. J Pharmacol Exp Ther, 1997, 283(2): 918-924.
| Cas No. | 112924-45-5 | SDF | |
| Chemical Name | (6aS,10aS)-9-(hydroxymethyl)-6,6-dimethyl-3-(2-methyloctan-2-yl)-6a,7,10,10a-tetrahydro-6H-benzo[c]chromen-1-ol | ||
| Canonical SMILES | OC1=C2[C@@H]3[C@H](CC=C(CO)C3)C(C)(C)OC2=CC(C(C)(C)CCCCCC)=C1 | ||
| Formula | C25H38O3 | M.Wt | 386.57 |
| Solubility | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:2): .25 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5869 mL | 12.9343 mL | 25.8685 mL |
| 5 mM | 0.5174 mL | 2.5869 mL | 5.1737 mL |
| 10 mM | 0.2587 mL | 1.2934 mL | 2.5869 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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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