Licostinel (Synonyms: ACEA-1021; CGP-63446; ACEA 1021; ACEA1021; CGP 63446) |
Catalog No.GF20364
One-Click Copy Product Info
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Licostinel is a glutamate receptor antagonist. Licostinel protects against permanent focal cerebral ischemia.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 153504-81-5
Sample solution is provided at 25 µL, 10mM.
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Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity.
| Animal Model: | The permanent model of middle cerebral artery occlusion in fisher 344 rats and CD-1 mice. The transient model of focal ischemia in Wistar and Sprague 鈥揇awley rats[2 |
| Dosage: | 5 mg/kg bolus 3.5 mg/kg/h for 6h, 10 mg/kg bolus 7.0 mg/kg/h for 6h |
| Administration: | A single intravenous injection bolus continuous infusion |
| Result: | Decreased infarct size. |
| Animal Model: | Male Sprague-Dawley rats [3] |
| Dosage: | 20, 40, 80 mg/kg for intraperitoneal injection (i.p.) bolus 7 mg/kg/h , 30mins |
| Administration: | Intravenous injection (i.v.) bolus continuous infusion |
| Result: | Reduced the rate of spreading depression and EEG activity in the rat brain in a dose-dependent manner. |
[1]. Zhou ZL, et al. Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists. Bioorg Med Chem. 2003 Apr 17;11(8):1769-80.
[2]. Albers GW, et al. Dose escalation study of the NMDA glycine-site antagonist licostinel in acute ischemic stroke. Stroke. 1999 Mar;30(3):508-13.
[3]. Martin H, et al. Effects of glycine receptor antagonism on spreading depression in the rat. Neurosci Lett. 1994 Oct 24;180(2):285-9.
| Cas No. | 153504-81-5 | SDF | |
| Synonyms | ACEA-1021; CGP-63446; ACEA 1021; ACEA1021; CGP 63446 | ||
| Formula | C8H3Cl2N3O4 | M.Wt | 276.03 |
| Solubility | DMSO : 12.5 mg/mL (45.28 mM; ultrasonic and warming and heat to 60°C) | Storage | 2-8°C; sealed storage; away from moisture |
| 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 | 3.6228 mL | 18.114 mL | 36.2279 mL |
| 5 mM | 724.6 μL | 3.6228 mL | 7.2456 mL |
| 10 mM | 362.3 μL | 1.8114 mL | 3.6228 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 solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)