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Purity: ≥98%
Loreclezole (R-72063; R 72063; R72063), a triazole analog, is a sedative, anti-seizure/anticonvulsant and antiepileptic agent that acts as a positive allosteric modulator (PAM) of GABAA receptor. Loreclezole has anti-seizure activity in a variety of seizure models, acting more like a barbiturate than a benzodiazepine in that the increase in seizure threshold produced by loreclezole was potentiated rather than blocked by the benzodiazepine antagonist, flumazenil, confirming that loreclezole does not interact with the benzodiazepine recognition site. In animal seizure models, loreclezole is protective against pentylenetetrazol seizures but is less active in the maximal electroshock test.
| ln Vivo |
Loreclezole (10, 25, 50, or 75 mg/kg, administered intraperitoneally 60 minutes before epileptic threshold measurement) induced a dose-dependent rise in epileptic threshold, as determined by the dose of pentylenetetrazole necessary to trigger convulsion 60 minutes later. Loreclezole also has negligible effects on loss of muscle tone, as evaluated by the "Pull-Up" test [3].
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| Animal Protocol |
Animal/Disease Models: Adult male Lister Hooded rat[3].
Doses: 10, 25, 50 or 75 mg/kg. Route of Administration: IP, 60 minutes before measuring seizure threshold. Experimental Results: Produced a dose-dependent increase in epileptic threshold, as measured by the dose of pentylenetetrazole required to produce convulsion after 60 minutes. |
| References |
[1]. Wingrove PB, et al. The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta 2 and beta 3 subunit. Proc Natl Acad Sci U S A. 1994 May 10;91(10):4569-73.
[2]. Sanna E, et al. Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60. [3]. Green AR, et al. A behavioural and neurochemical study in rats of the pharmacology of loreclezole, a novel allosteric modulator of the GABAA receptor. Neuropharmacology. 1996;35(9-10):1243-50. |
| Molecular Formula |
C10H6CL3N3
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|---|---|
| Molecular Weight |
274.52
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| Exact Mass |
272.9627
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| CAS # |
117857-45-1
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| Related CAS # |
117857-45-1;2227372-56-5 (HCl);
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| SMILES |
ClC1=CC=C(/C(Cl)=C/N2N=CN=C2)C(Cl)=C1.[H]Cl
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| Chemical Name |
(Z)-1-(2-chloro-2-(2,4-dichlorophenyl)vinyl)-1H-1,2,4-triazole
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| Synonyms |
R-72063 R 72063 R72063
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~110 mg/mL (~400.68 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6427 mL | 18.2136 mL | 36.4272 mL | |
| 5 mM | 0.7285 mL | 3.6427 mL | 7.2854 mL | |
| 10 mM | 0.3643 mL | 1.8214 mL | 3.6427 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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