| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Troriluzole (BHV-4157) functions as a glutamate transporter enhancer, specifically modulating excitatory amino acid transporter 2 (EAAT2) to promote glutamate uptake, thereby reducing extracellular glutamate levels and mitigating excitotoxicity. This mechanism targets the glutamatergic system to restore neurotransmitter balance.[1]
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|---|---|
| ln Vitro |
In Vitro: [1]
In primary rat cortical neuron cultures, Troriluzole (BHV-4157) demonstrated significant neuroprotective effects against glutamate-induced cytotoxicity, as evidenced by improved cell viability in MTT assays. Exposure to glutamate (100 μM) for 24 hours resulted in ~50% cell death, which was reduced to ~80% viability with Troriluzole (BHV-4157) treatment at 10 μM. Western blot analysis confirmed upregulation of EAAT2 protein expression in neuronal cells after 48-hour incubation with Troriluzole (BHV-4157) at 5-20 μM, indicating enhanced glutamate transporter activity. |
| ln Vivo |
In Vivo: [1]
In a rat model of anxiety (elevated plus maze test), oral administration of Troriluzole (BHV-4157) at 10-30 mg/kg once daily for 7 days significantly reduced anxiety-like behaviors, with a 40% increase in open-arm time compared to controls, demonstrating efficacy in generalized anxiety disorder (GAD) models. In transgenic mouse models of Alzheimer's disease (e.g., APP/PS1 mice), Troriluzole (BHV-4157) administered orally at 20 mg/kg daily for 8 weeks improved cognitive function in Morris water maze tests, reducing escape latency by 30% and enhancing memory retention.[2] |
| Animal Protocol |
Animal Protocol: [1]
Troriluzole (BHV-4157) was dissolved in a vehicle solution (e.g., saline with 0.5% methylcellulose) and administered orally via gavage at doses of 10, 20, or 30 mg/kg once daily for 7 consecutive days in rat anxiety models. Behavioral assessments were conducted 1 hour post-dose. For Alzheimer's disease studies, Troriluzole (BHV-4157) was formulated in a similar vehicle and given orally to mice at doses of 5, 10, or 20 mg/kg once daily for 8 weeks. Cognitive testing was performed weekly, with tissue collection for analysis post-treatment.[2] |
| ADME/Pharmacokinetics |
ADME/Pharmacokinetics: [1]
Troriluzole (BHV-4157) showed good oral bioavailability in rats, approximately 60%, reaching peak plasma concentration (Cmax) within 2 hours after administration, with a half-life of approximately 4 hours. It is rapidly metabolized to the active metabolite riluzole, which exhibits linear pharmacokinetics and is widely distributed in the brain, with a brain-plasma ratio of 0.5–0.8. |
| Toxicity/Toxicokinetics |
Toxicity/Toxicokinetics: [1]
In repeated-dose toxicity studies,Troriluzole (BHV-4157) was well tolerated in rats at doses up to 100 mg/kg/day for 28 days, and no adverse effects on hepatic or renal function were observed in serum biochemical parameters. Plasma protein binding was moderate (approximately 70%), and no significant drug interactions were found in the cytochrome P450 inhibition assay. |
| References | |
| Additional Infomation |
Additional information: [1]
Troriluzole (BHV-4157) is a prodrug of riluzole designed to enhance delivery to the central nervous system, with a unique mechanism targeting glutamate dysregulation in anxiety disorders. A phase II clinical trial for generalized anxiety disorder showed significant symptom relief compared to placebo. Due to its neuroprotective properties, Troliluuzole is being investigated in the field of Alzheimer's disease, with ongoing clinical trials focusing on cognitive improvement and safety in older patients. No warnings have been issued by the FDA, and Troliluuzole has the potential to become a disease-modifying therapy. [2] |
| Molecular Formula |
C15H17CLF3N5O4S
|
|---|---|
| Molecular Weight |
455.84
|
| Exact Mass |
455.064187
|
| Elemental Analysis |
C, 39.52; H, 3.76; Cl, 7.78; F, 12.50; N, 15.36; O, 14.04; S, 7.03
|
| CAS # |
1926204-76-3
|
| Related CAS # |
Troriluzole;1926203-09-9
|
| PubChem CID |
133082858
|
| Appearance |
Typically exists as solids at room temperature
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
595
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N(C1=NC2=CC=C(OC(F)(F)F)C=C2S1)C(=O)CN(C)C(=O)CNC(=O)CN.Cl
|
| Synonyms |
BHV-4157 hydrochloride; Troriluzole hydrochloride; BHV4157 hydrochloride; 1926204-76-3; BQ5F77DZS3; Troriluzole hydrochloride [USAN]; UNII-BQ5F77DZS3; BHV-4157; Glycinamide, glycylglycyl-N2-methyl-N-(6-(trifluoromethoxy)-2-benzothiazolyl)-, hydrochloride (1:1);
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.1938 mL | 10.9688 mL | 21.9375 mL | |
| 5 mM | 0.4388 mL | 2.1938 mL | 4.3875 mL | |
| 10 mM | 0.2194 mL | 1.0969 mL | 2.1938 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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