JW-65
Based on 1 Customer Validation
JW-65 is a selective TRPC3 channel inhibitor with favorable blood-brain barrier penetration. JW-65 directly binds to human TRPC3 protein and modulates calcium signaling to reduce seizure susceptibility. JW-65 reduces seizure incidence, severity, and duration while prolonging seizure latency in multiple seizure models. JW-65 alleviates Aβ‑induced neuronal damage. JW-65 serves as a valuable tool for research on epilepsy, seizure disorders, and Alzheimer’s disease.
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- 純度: 99.05%
- CAS 番号: 2763378-71-6
- 分子式: C18H13Cl2F3N4O2
- 分子量:445.22
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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TRPC3 0.37 μM (IC50) |
JW-65 (0.001-10 μM) potently inhibits hTRPC3-mediated currents in HEK293 cells, with IC50 values of 0.37 μM (no extracellular Ca2+)[2].
JW-65 (10 μM) is a selective inhibitor of hTRPC3 over other TRP channel family members, showing no inhibition of hTRPA1, rTRPV1, rTRPV4, or hTRPM8, and only partial inhibition of closely related hTRPC6 (39%) and hTRPC7 (26%) at 10 μM[2].
JW-65 exhibits significantly improved metabolic stability over Pyr3 (HY-108465), with a half-life of more than 4 hours in mouse, rat, and human liver microsomes[2][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | T1/2 |
|---|---|---|---|---|---|
| Mice[3] | 100 mg/kg | i.p. | 156 ng/mL | 0.33 h | 3.1 h |
JW-65 (10 mg/kg; i.p.; daily; 5 consecutive days) completely suppress acoustically-evoked seizures in male and female GEPR-3 rats[1].
Pretreatment with JW-65 (100 mg/kg; i.p.; once daily for 2 consecutive days, plus a third dose on experiment day 15 minutes before Pilocarpine (HY-B0726A) injection) substantially impairs the initiation and development of Pilocarpine-induced status epilepticus in mice[3].
Post-seizure onset treatment with JW-65 (100 mg/kg; i.p.; single dose administered after Stage 2 seizure onset) mitigates the progression of Pilocarpine-induced status epilepticus in mice, preventing all treated mice from developing long-lasting status epilepticus and reducing electrographic seizure activity[3].
JW-65 (20-100 mg/kg; i.p.; single dose 30 minutes before PTZ injection) reduces susceptibility to PTZ-induced seizures in mice in a dose-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Genetically Epilepsy-Prone Rats (GEPR-3) (adult male and female, 8 weeks old)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:i.p.; single dose
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Result:Reduced seizure duration in males at 5 mg/kg without altering other seizure parameters in either sex.
Dose-dependently decreased WRS and GTCS incidence, prolonged latency, shortened duration, and reduced severity at 10, 20, and 40 mg/kg in both sexes, with stronger effects in females.
Impaired seizure activity most potently at 40 mg/kg, with maximal inhibition of GTCS (89%) in females.
Induced mild neurological side effects only at 40 mg/kg, and was well-tolerated at 5-20 mg/kg.
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Animal Model:Genetically Epilepsy-Prone Rats (GEPR-3) (adult male and female, 8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 5 consecutive days
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Result:Completely suppressed WRS and GTCS incidence, duration, and severity in both sexes at 0.5-4 h after the last treatment; seizure susceptibility recovered to baseline at 24 h.
Markedly prolonged seizure latency in both sexes at 0.5-4 h after the last treatment.
Significantly reduced seizure duration in females but not males at 24 h after the last treatment.
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Animal Model:C57BL/6 (young adult male, 8-10 weeks, pilocarpine-induced status epilepticus, pretreated with methylscopolamine and terbutaline prior to pilocarpine injection)[3]
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Dosage:100 mg/kg
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Administration:i.p.; once daily for 2 consecutive days, plus a third dose on experiment day 15 minutes before pilocarpine injection
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Result:Markedly reduced overall behavioral seizure scores.
Prolonged latencies to Stage 2, 3, and 4 seizures with high statistical significance.
Decreased both average and maximal seizure scores.
Dramatically lowered the incidence of status epilepticus.
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Animal Model:C57BL/6 (young adult male, 8-10 weeks, pilocarpine-induced status epilepticus, pretreated with methylscopolamine and terbutaline prior to pilocarpine injection, treatment administered after seizure onset)[3]
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Dosage:100 mg/kg
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Administration:i.p.; single dose administered after Stage 2 seizure onset
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Result:Reduced overall behavioral seizure scores.
Prolonged latencies to Stage 3 and Stage 4 seizures significantly.
Lowered both average and maximal seizure scores.
Blocked long-lasting status epilepticus in all treated mice.
Elevated survival rate to 88.8% from 53.8% in vehicle controls.
Decreased EEG spike counts time-dependently within 4 hours.
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Animal Model:C57BL/6 (young adult male, 8-10 weeks, pentylenetetrazole-induced seizures)[3]
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Dosage:20 mg/kg; 100 mg/kg
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Administration:i.p.; single dose 30 minutes before PTZ injection
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Result:Lowered the proportion of mice exhibiting myoclonic jerks (MJ) and prolonged MJ latency at 20 mg/kg.
Reduced the incidence of both MJ and GTCS in mice at 100 mg/kg.
Markedly delayed the onset of initial MJ and GTCS at 100 mg/kg, with efficacy similar to phenytoin.
化学情報
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CAS 番号 2763378-71-6
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性状 Solid
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分子量 445.22
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分子式 C18H13Cl2F3N4O2
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Color White to off-white
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SMILES
FC(C1=C(C(NCC)=O)C=NN1C2=CC=C(C=C2)N(C=CC(Cl)=C3Cl)C3=O)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 25 mg/mL (56.15 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Silva-Cardoso GK, et al. Inhibition of TRPC3 channels suppresses seizure susceptibility in the genetically-epilepsy prone rats. Eur J Pharmacol. 2024;977:176722. [Content Brief]
[2]. Zhang S, et al. Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. ACS Med Chem Lett. 2021;12(4):572-578. Published 2021 Mar 5. [Content Brief]
[3]. Nagib MM, et al. Inhibition of TRPC3 channels by a novel pyrazole compound confers antiseizure effects. Epilepsia. 2022;63(4):1003-1015. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2461 mL | 11.2304 mL | 22.4608 mL | 56.1520 mL |
| 5 mM | 0.4492 mL | 2.2461 mL | 4.4922 mL | 11.2304 mL | |
| 10 mM | 0.2246 mL | 1.1230 mL | 2.2461 mL | 5.6152 mL | |
| 15 mM | 0.1497 mL | 0.7487 mL | 1.4974 mL | 3.7435 mL | |
| 20 mM | 0.1123 mL | 0.5615 mL | 1.1230 mL | 2.8076 mL | |
| 25 mM | 0.0898 mL | 0.4492 mL | 0.8984 mL | 2.2461 mL | |
| 30 mM | 0.0749 mL | 0.3743 mL | 0.7487 mL | 1.8717 mL | |
| 40 mM | 0.0562 mL | 0.2808 mL | 0.5615 mL | 1.4038 mL | |
| 50 mM | 0.0449 mL | 0.2246 mL | 0.4492 mL | 1.1230 mL |
JW-65 関連分類
HY-138668 関連分類
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