| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
Voltage-gated sodium channels (VGSCs) [1][2]
N-methyl-D-aspartate (NMDA) receptors (potential target) [1][2] |
|---|---|
| ln Vivo |
Neuropathic pain is suppressed by ralfinamide (80 mg/kg; oral; twice daily; 7 days) used as a preoperative therapy [1].
In rats subjected to hindpaw neurectomy, oral administration of Ralfinamide mesylate (doses: 30, 60, 120 mg/kg) either 1 hour before surgery or postoperatively (starting 24 hours after surgery) produced long-lasting suppression of spontaneous neuropathic pain-related behaviors (e.g., paw licking, biting, and shaking). The analgesic effect was significant at doses ≥60 mg/kg and persisted for up to 21 days post-surgery, with no tolerance development observed. [1] In rats with chronic constriction injury (CCI) of the sciatic nerve (nerve injury model), oral Ralfinamide mesylate (doses: 30, 60 mg/kg) dose-dependently inhibited mechanical allodynia and thermal hyperalgesia, with the 60 mg/kg dose exerting a significant analgesic effect lasting for 4-6 hours. [2] In a paclitaxel-induced chemotherapy-induced neuropathic pain model (rats injected intraperitoneally with paclitaxel), oral Ralfinamide mesylate (doses: 30, 60 mg/kg) significantly reversed mechanical allodynia and thermal hyperalgesia without affecting the rats' body weight or general locomotor activity. [2] |
| Animal Protocol |
Animal/Disease Models: 81 adult male SD (SD (Sprague-Dawley)) rats (260-460 g) [1]
Doses: 80 mg/kg (7 days before surgery), 30 mg/kg, 60 mg/kg (after surgery) twice a day times; until the 42nd postoperative day. Experimental Results: Neuropathic pain was suppressed. Hindpaw neurectomy model for spontaneous neuropathic pain: Adult rats were anesthetized, and the common peroneal and tibial nerves of the right hindpaw were transected to establish the neuropathic pain model. Ralfinamide mesylate was dissolved in a suitable vehicle (e.g., physiological saline with a small amount of solubilizer) and administered via oral gavage. Two administration regimens were used: pre-surgical (1 hour before neurectomy) or post-surgical (starting 24 hours after neurectomy, once daily for 7 consecutive days). Pain-related behaviors (paw licking, biting, shaking frequency and duration) were recorded daily for up to 21 days post-surgery. [1] Chronic constriction injury (CCI) model for nerve injury-induced pain: Adult rats were anesthetized, and the right sciatic nerve was loosely ligated with sutures to induce neuropathic pain. Ralfinamide mesylate was administered via oral gavage at doses of 30 and 60 mg/kg, once daily for 5 consecutive days starting 7 days after CCI surgery. Mechanical allodynia (assessed by von Frey filaments) and thermal hyperalgesia (assessed by plantar test) were measured before and after drug administration. [2] Paclitaxel-induced chemotherapy-induced neuropathic pain model: Adult rats were injected intraperitoneally with paclitaxel on days 0, 2, 4, and 6 to induce neuropathic pain. From day 7 onwards, Ralfinamide mesylate was administered via oral gavage at doses of 30 and 60 mg/kg, once daily for 7 consecutive days. Mechanical allodynia, thermal hyperalgesia, and body weight were monitored throughout the experiment. [2] |
| Toxicity/Toxicokinetics |
Lafenamide mesylate did not cause significant toxicity in rats within a dose range of 30–120 mg/kg (orally). No abnormalities were observed in general behavior, food intake, or body weight in rats, nor was there any evidence of drug-related organ damage or death. [1][2]
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| References |
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| Additional Infomation |
Lafilamide mesylate is a novel drug for the treatment of neuropathic pain. Its mechanism of action may involve inhibition of voltage-gated sodium channels (particularly persistent sodium currents) and modulation of N-methyl-D-aspartate (NMDA) receptors or GABAergic neurotransmission. [1][2] The analgesic effect of lamivamethanesylate is persistent (lasting up to 21 days in a hind claw neurectomy model) and tolerability-free, making it an ideal candidate for the treatment of chronic neuropathic pain. [1] In a chemotherapy-induced neuropathic pain model, lamivamethanesylate effectively relieved pain without interfering with the antitumor effect of paclitaxel (indirectly confirmed by no changes in weight and overall health status), indicating a good safety profile when used in combination with chemotherapy drugs. [2]
|
| Molecular Formula |
C17H19N2O2F.CH4O3S
|
|---|---|
| Molecular Weight |
398.44902
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| Exact Mass |
398.131
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| CAS # |
202825-45-4
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| Related CAS # |
Ralfinamide;133865-88-0
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| PubChem CID |
23661379
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.044
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
438
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](NCC1=CC=C(OCC2=CC=CC=C2F)C=C1)C(N)=O.CS(=O)(O)=O
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| InChi Key |
CHQVNINIGBRKGZ-YDALLXLXSA-N
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| InChi Code |
InChI=1S/C17H19FN2O2.CH4O3S/c1-12(17(19)21)20-10-13-6-8-15(9-7-13)22-11-14-4-2-3-5-16(14)18;1-5(2,3)4/h2-9,12,20H,10-11H2,1H3,(H2,19,21);1H3,(H,2,3,4)/t12-;/m0./s1
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| Chemical Name |
(2S)-2-[[4-[(2-fluorophenyl)methoxy]phenyl]methylamino]propanamide;methanesulfonic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5097 mL | 12.5486 mL | 25.0973 mL | |
| 5 mM | 0.5019 mL | 2.5097 mL | 5.0195 mL | |
| 10 mM | 0.2510 mL | 1.2549 mL | 2.5097 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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