| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Glutamatergic system modulator (exact targets not quantified)[1][2]
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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. Systemic absorption of troruzole results in its cleavage to riluzole by aminopeptidase [1]. |
| 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 |
Troriluzole is being investigated in the clinical trial NCT03701399 (Troriluzole for the treatment of spinocerebellar ataxia in adults). Troriluzole is a formulation consisting of a prodrug form of the benzothiazole derivative riluzole, possessing potential antidepressant, anti-anxiety, and antitumor activities. After oral administration, Troriluzole is converted to its active form, riluzole. While the mechanism of action of riluzole is not fully understood, its pharmacological activities (some of which may be related to its effects) include: 1) inhibition of glutamate release; 2) inactivation of voltage-dependent sodium channels; and 3) interference with intracellular events following the binding of neurotransmitters to excitatory amino acid receptors. These activities may lead to muscle relaxation and sedation by blocking glutamatergic neurotransmission. Furthermore, these activities may inhibit enzymes required for cell growth, thereby reducing tumor cell growth and metastasis.
Additional Information: [1] Troriluzole (BHV-4157) is a prodrug of riluzole designed to enhance drug delivery in the central nervous system. Its unique mechanism targets 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 for Alzheimer's disease, with ongoing clinical trials focusing on cognitive improvement and safety in older patients. The FDA has not issued any warnings, and Troliluuzole has the potential to become a disease-modifying therapy. |
| Molecular Formula |
C15H16F3N5O4S
|
|---|---|
| Molecular Weight |
419.3792
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| Exact Mass |
419.087
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| Elemental Analysis |
C, 42.96; H, 3.85; F, 13.59; N, 16.70; O, 15.26; S, 7.64
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| CAS # |
1926203-09-9
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| PubChem CID |
121488186
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.612
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| LogP |
1.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
595
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=NC2C([H])=C([H])C(=C([H])C1=2)OC(F)(F)F)N([H])C(C([H])([H])N(C([H])([H])[H])C(C([H])([H])N([H])C(C([H])([H])N([H])[H])=O)=O)=O
|
| InChi Key |
YBZSGIWIPOUSHY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H16F3N5O4S/c1-23(13(26)6-20-11(24)5-19)7-12(25)22-14-21-9-3-2-8(4-10(9)28-14)27-15(16,17)18/h2-4H,5-7,19H2,1H3,(H,20,24)(H,21,22,25)
|
| Chemical Name |
2-amino-N-[2-[methyl-[2-oxo-2-[[6-(trifluoromethoxy)-1,3-benzothiazol-2-yl]amino]ethyl]amino]-2-oxoethyl]acetamide
|
| Synonyms |
troriluzole; Trigriluzole; BHV-4157a; BHV4157; Troriluzole [USAN]; S7H48S6K7H; BHV-4157; UNII-S7H48S6K7H; ...; 1926203-09-9;BHV-4157
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~119.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.96 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 (5.96 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3845 mL | 11.9224 mL | 23.8447 mL | |
| 5 mM | 0.4769 mL | 2.3845 mL | 4.7689 mL | |
| 10 mM | 0.2384 mL | 1.1922 mL | 2.3845 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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