| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Voltage-Gated Sodium Channels (NaV) (sodium channel)
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| ln Vitro |
Bliretrigine is a sodium channel blocker. It inhibits voltage-gated sodium channels to reduce neuronal excitability and provide pain relief. It is described as having "the effect of relieving pain." No specific IC50 values or isoform selectivity data are publicly available, but it is characterized as a potent blocker.
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| ln Vivo |
No specific in vivo data for Bliretrigine in the provided search results, though the compound is described as having "the effect of relieving pain." As a sodium channel blocker, it would be expected to have analgesic efficacy in animal models of pain (e.g., formalin test, CFA-induced inflammatory pain, or nerve injury-induced neuropathic pain). In vivo studies would involve oral or intraperitoneal administration to rodents to assess pain behavior.
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| Enzyme Assay |
No specific enzyme/receptor binding protocol available. As a sodium channel blocker, the binding affinity would typically be assessed using radioligand binding assays with [3H]saxitoxin or [3H]batrachotoxin on purified NaV channels from brain tissue. Alternatively, automated patch-clamp systems using HEK293 cells expressing specific NaV isoforms can be used to determine IC50 values at various holding potentials to assess state-dependent block.
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| Cell Assay |
For cellular assays, HEK293 cells or ND7/23 cells expressing human NaV isoforms (e.g., NaV1.7, NaV1.8) are cultured in DMEM with 10% FBS. Whole-cell patch-clamp recordings are performed to measure sodium currents. Cells are held at a depolarized potential (e.g., -60 mV) to mimic inactivated channel states. Bliretrigine is perfused at varying concentrations (0.1-100 uM), and current inhibition is measured. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
No specific in vivo animal study data available. A typical protocol for assessing in vivo analgesic efficacy would involve administering Bliretrigine (e.g., 1-30 mg/kg) via oral gavage or intraperitoneal injection to male Sprague-Dawley rats or ICR mice. Pain models would include the formalin-induced paw licking test, CFA-induced thermal hyperalgesia (Hargreaves test), or chronic constriction injury (CCI) model for neuropathic pain. Behavioral responses are measured for 60-180 min post-administration.
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| ADME/Pharmacokinetics |
No specific PK data for Bliretrigine. As a small molecule sodium channel blocker (MW 352.43), it would likely be orally bioavailable with moderate half-life. The structure suggests moderate lipophilicity, which may allow CNS penetration for central pain pathways. Detailed PK parameters (Cmax, Tmax, AUC, half-life) would need to be determined experimentally. The compound is typically formulated in DMSO for in vitro studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Bliretrigine. As a sodium channel blocker, potential on-target toxicities include CNS effects (dizziness, sedation, ataxia) and cardiovascular effects (QT prolongation, arrhythmias). Preclinical safety studies would typically include hERG channel inhibition assays, CYP450 inhibition screening, and acute toxicity studies in rodents. For research use, handle with standard precautions (gloves, lab coat, eye protection).
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| References | |
| Additional Infomation |
Bliretrigine is a small molecule drug. The international nonproprietary name stem "-trigine" in its name indicates that bliretrigine is a sodium channel blocker and signal transduction modulator. The monoisotopic molecular weight of bliretrigine is 352.19 Da.
Bliretrigine (CAS: 1233229-75-8) is a research compound used for studying sodium channel biology and as a potential analgesic. The compound has the molecular formula C20H24N4O2 and molecular weight 352.43. It is soluble in DMSO (10 mM stock). It is not approved for clinical use and is for research purposes only. References: Patent applications (e.g., WO2012112710A2) and associated literature describe sodium channel blockers for pain. |
| Molecular Formula |
C20H24N4O2
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|---|---|
| Molecular Weight |
352.430164337158
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| Exact Mass |
352.189
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| CAS # |
1233229-75-8
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| PubChem CID |
46701178
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
467
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C1C=CC(C)=CC=1)C1C=CC2=C(C=1)N(CC)C(CN[C@H](C(N)=O)C)=N2
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| InChi Key |
ZYUAASICHDTDEK-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C20H24N4O2/c1-4-24-18-11-16(26-15-7-5-13(2)6-8-15)9-10-17(18)23-19(24)12-22-14(3)20(21)25/h5-11,14,22H,4,12H2,1-3H3,(H2,21,25)/t14-/m0/s1
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| Chemical Name |
(2S)-2-[[1-ethyl-6-(4-methylphenoxy)benzimidazol-2-yl]methylamino]propanamide
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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 (141.87 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.09 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 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 (7.09 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8374 mL | 14.1872 mL | 28.3744 mL | |
| 5 mM | 0.5675 mL | 2.8374 mL | 5.6749 mL | |
| 10 mM | 0.2837 mL | 1.4187 mL | 2.8374 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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