| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The exact target of Carisbamate is not fully elucidated, but it is known to be a neuromodulator. It produces anticonvulsant effects in various seizure models and exhibits neuroprotective and antiepileptogenic properties in rodent epilepsy models.
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|---|---|
| ln Vitro |
In vitro studies confirm the compound's neuromodulatory properties. The specific in vitro activity of the (R)-enantiomer is expected to be similar to the racemic mixture, though enantiomers can have differing potencies. Its activity is typically measured in neuronal cell models of hyperexcitability.
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| ln Vivo |
In vivo, (R)-Carisbamate is the active isomer of Carisbamate. Carisbamate produces anticonvulsant effects in primary generalized, complex partial, and absence-type seizure models. This suggests that the R-isomer is responsible for the therapeutic effects observed with the racemic mixture.
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| Enzyme Assay |
In vitro receptor binding or enzyme assays are not the primary methods for studying Carisbamate's mechanism. Its activity is typically assessed in functional assays that measure neuronal excitability, such as patch-clamp electrophysiology on cultured neurons.
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| Cell Assay |
In vitro cell-based assays involve using neuronal cell cultures to study the compound's effects on seizure-like activity. This can include measuring changes in intracellular calcium levels, neuronal firing rates, or the expression of genes related to neuronal excitability.
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| Animal Protocol |
The in vivo anticonvulsant activity is evaluated in standard rodent seizure models, including maximal electroshock (MES) and pentylenetetrazol (PTZ) tests. The compound is administered orally, and its ability to prevent or reduce the severity of seizures is measured.
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| ADME/Pharmacokinetics |
As an orally active neuromodulator, (R)-Carisbamate is designed for convenient administration. Its pharmacokinetic properties are suitable for achieving therapeutic concentrations in the brain to exert its anticonvulsant effects.
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| Toxicity/Toxicokinetics |
The toxicological profile of (R)-Carisbamate is likely similar to that of the racemic Carisbamate. As an experimental drug, its safety has been evaluated in preclinical and clinical studies. Common side effects are expected to be related to its central nervous system activity.
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| References |
:J Clin Pharmacol. 2012 Sep;52(9):1420-9.
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| Additional Infomation |
(R)-Carisbamate is the active enantiomer of the anticonvulsant drug Carisbamate. The development of the single enantiomer was likely pursued to improve the therapeutic index or pharmacokinetic profile compared to the racemic mixture. It is not an FDA-approved drug.
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| Molecular Formula |
C9H10CLNO3
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|---|---|
| Molecular Weight |
215.633
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| Exact Mass |
215.035
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| CAS # |
194085-74-0
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| Related CAS # |
194085-75-1 (S-isomer);194085-74-0 (R-isomer);
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| PubChem CID |
9942577
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| Appearance |
White to off-white solid
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| LogP |
1.982
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
201
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C(C(=C1)C(COC(=O)N)O)Cl
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| InChi Key |
OLBWFRRUHYQABZ-QMMMGPOBSA-N
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| InChi Code |
InChI=1S/C9H10ClNO3/c10-7-4-2-1-3-6(7)8(12)5-14-9(11)13/h1-4,8,12H,5H2,(H2,11,13)/t8-/m0/s1
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| Chemical Name |
[(2R)-2-(2-chlorophenyl)-2-hydroxyethyl] carbamate
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| Synonyms |
(R)-YKP509; JNJ10234094; (R)-YKP-509; (R)-YKP 509; JNJ10234094; JNJ-10234094; trade name Comfyde.
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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: ~100 mg/mL (~463.8 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (11.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (11.59 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6376 mL | 23.1879 mL | 46.3757 mL | |
| 5 mM | 0.9275 mL | 4.6376 mL | 9.2751 mL | |
| 10 mM | 0.4638 mL | 2.3188 mL | 4.6376 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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