| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Benzodiazepine receptor; Schistosoma mansoni (parasite).
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| ln Vitro |
In young Salmonella mansoni, clonazepam first results in severe spastic paralysis [2].
Meclonazepam (30 µM) eliminates 100% of immature S. mansoni parasites. It causes initially a massive spastic paralysis of immature S. mansoni. The compound has anti-schistosomal effects. Meclonazepam does not compete with praziquantel for the same binding sites in schistosomes. |
| ln Vivo |
In gerbils, meclonazepam (0.1–5.6 mg/kg) exhibits anxiolytic effects [1]. The effects of clonazepam (40 and 80 mg/kg) on immature schistosomiasis are highly notable [2].
Meclonazepam (0.1-5.6 mg/kg) exhibits anxiolytic effect in gerbils. Meclonazepam (40 and 80 mg/kg) has highly significant effect on immature schistosomes. |
| Enzyme Assay |
In vitro assays for anti-schistosomal activity use immature S. mansoni parasites cultured in suitable medium. Meclonazepam is added at concentrations ranging from 0.1-100 µM. Parasite viability is assessed by microscopic examination of motility and morphology at various time points (24-72 hours). The percentage of parasite elimination is calculated. For receptor binding, radioligand displacement assays using [3H]flunitrazepam and brain membrane preparations are performed.
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| Cell Assay |
In vitro cellular assays are performed using parasite cultures or mammalian cell lines. Schistosomula or adult schistosomes are incubated with Meclonazepam (0.1-100 µM) for 24-72 hours. Parasite viability is assessed by vital dye exclusion (e.g., methylene blue) or by measuring ATP levels. For anxiolytic activity, GABA-A receptor modulation is assessed in neuronal cell cultures using electrophysiological or calcium imaging techniques. Cytotoxicity is evaluated in mammalian cell lines.
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| Animal Protocol |
Animal/Disease Models: Adult experimental naive male Mongolian gerbil (Meriones unguiculatus) [1]
Doses: 0.1, 0.3, 1.0, 3.0, 5.6 mg/kg Route of Administration: intraperitonealadministration 5 minutes before the start of training. Experimental Results: ED50 5 minutes post injection (pi) was 0.77-0.78 mg/kg. Animal/Disease Models: CB6F1 mice infected with single-sex male Salmonella mansoni cercariae 28 days before treatment [2] Doses: 40 and 80 mg/kg Route of Administration: administered by gavage, either as a single agent or as a A sequence of 1 dose of praziquantel (PZQ) was administered 5 minutes apart, followed by a dose of Ro followed by a 15 minute interval between the second dose of PZQ. Experimental Results: PZQ had no obvious effect on immature schistosomiasis, while Ro 11-3128 was highly effective. In vivo efficacy is evaluated in mouse models of schistosomiasis. Mice infected with S. mansoni cercariae are treated with Meclonazepam orally at doses of 10-80 mg/kg. Worm burden is assessed by perfusion of the portal system. Egg counts are determined in liver and intestinal tissues. For anxiolytic activity, the elevated plus maze or open field tests are used in gerbils or mice following oral administration. |
| ADME/Pharmacokinetics |
Meclonazepam has a molecular weight of 329.74 g/mol and molecular formula C16H12ClN3O3. Store at room temperature in continental US; may vary elsewhere. Soluble in DMSO. Purity ≥98%. For in vivo studies, formulate in suitable vehicle (e.g., PEG400 or saline with appropriate solubilizers).
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for Meclonazepam. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments for benzodiazepines would include assessment of sedation, motor coordination impairment, and dependence potential. The compound is for research use only and not for human therapeutic use.
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| References |
[1]. T U Järbe, et al. Cueing effects of anxiolytic benzodiazepines (DZP and Ro 11-3128): stereospecificity and antagonism by the convulsant benzodiazepine Ro 5-3663. Psychopharmacology (Berl). 1988;94(4):501-6.
[2]. L Pica-Mattoccia, et al. Praziquantel and the benzodiazepine Ro 11-3128 do not compete for the same binding sites in schistosomes. Parasitology. 2008 Jan;135(Pt 1):47-54. |
| Additional Infomation |
Meclonazepam is a research-grade benzodiazepine with both anxiolytic and anti-schistosomal activities. It is not approved for clinical use. Also known as Ro 11-3128. References include Järbe et al. (1988) and Pica-Mattoccia et al. (2008). It is a valuable tool for studying benzodiazepine pharmacology and schistosomiasis.
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| Molecular Formula |
C16H12CLN3O3
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|---|---|
| Molecular Weight |
329.74
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| Exact Mass |
329.057
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| CAS # |
58662-84-3
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| Related CAS # |
(R)-Meclonazepam;86630-81-1
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| PubChem CID |
3033985
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| Appearance |
White to off-white solid powder
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| Density |
1.46
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| Boiling Point |
522.1ºC at 760 mmHg
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| Flash Point |
269.6ºC
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| Index of Refraction |
1.686
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| LogP |
3.523
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
519
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=[N+](C1C=CC2=C(C(C3=CC=CC=C3Cl)=NC(C(N2)=O)C)C=1)[O-]
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| InChi Key |
LMUVYJCAFWGNSY-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C16H12ClN3O3/c1-9-16(21)19-14-7-6-10(20(22)23)8-12(14)15(18-9)11-4-2-3-5-13(11)17/h2-9H,1H3,(H,19,21)/t9-/m0/s1
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| Chemical Name |
(3S)-5-(2-chlorophenyl)-3-methyl-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one
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| Synonyms |
Ro 113128; Meclonazepamum; Meclonazepam
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| HS Tariff Code |
2934.99.9001
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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 : ~50 mg/mL (~151.63 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.58 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (7.58 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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 | 3.0327 mL | 15.1635 mL | 30.3269 mL | |
| 5 mM | 0.6065 mL | 3.0327 mL | 6.0654 mL | |
| 10 mM | 0.3033 mL | 1.5163 mL | 3.0327 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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