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Riluzole [1744-22-5]

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Referência NB-64-00516-100mg

Tamanho : 100mg

Marca : Neo Biotech

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Riluzole

(Synonyms: RP-54274, PK 26124) Copy Product Info

Synonyms: RP-54274, PK 26124

Catalog No. T0349 Copy Product Info

Purity: 99.88%

Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.

Cas No. 1744-22-5

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.88%

Color:White to Yellow

Product Information

Riluzole AI Summary

Riluzole exhibits a diverse range of bioactivities, indicating potential therapeutic applications across multiple domains. It functions as a sodium channel blocker with an IC50 of 4730 nM and a voltage-gated Ca2+ channel blocker in rat brain synaptosomes with an IC50 of 0.0 nM, showing potent inhibition of K+-evoked and veratridine-induced glutamate release. Additionally, Riluzole protects against seizures and has neuroprotective activity, demonstrated by efficacy in rat models of glutamate-induced convulsions (ED50 of 3.2 mg/kg) and focal stroke (effective at 4.0 mg/kg and 30.0 mg/kg). The compound shows considerable metabolic stability, liver enzyme modulation, and potential for therapeutic applications in neuroprotection and stroke. It has a partition coefficient (logD7.4) of 3.43, high plasma protein binding of 97.13%, and demonstrates moderate lipophilicity (LogP 3.2). Additionally, it interferes with various cellular processes, including mitochondrial function, NFkB signaling, and Lamin A splicing, and inhibits several enzymes like BSEP (IC50 139000 nM) and human UGT1A1. In terms of antibacterial and antifungal activity, Riluzole shows efficacy against Escherichia coli, Enterococcus faecalis, Staphylococcus aureus, and several Candida species. It also demonstrates antivirals by inhibiting SARS-CoV-2 3CL-Pro protease and virus-induced cytotoxicity in VERO-6 cells. Moreover, Riluzole has cytotoxic effects in some cell lines but displays neuroprotective properties against excitotoxic and oxidative stress in neuronal cells. Its high aqueous solubility, moderate passive permeability, and good liver microsomal stability underscore its potential as a drug candidate. Overall, Riluzole’s broad bioactivity profile underscores its potential for therapeutic development in treating neurological disorders, infectious diseases, and metabolic conditions..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
Targets & IC50	GABA:43 μM
In vitro	Riluzole readily crosses the blood-brain barrier. Treatment of rodents with transient cerebral ischemia with 8 mg/kg i.p. Riluzole completely inhibited the massive release of glutamic acid induced by local ischemia.
In vivo	Riluzole readily crosses the blood-brain barrier. Treatment of rodents with transient cerebral ischemia with 8 mg/kg i.p. Riluzole completely inhibited the massive release of glutamic acid induced by local ischemia.
Synonyms	RP-54274, PK 26124

Chemical Properties

Molecular Weight	234.198
Formula	C₈H₅F₃N₂OS
Cas No.	1744-22-5
Smiles	NC1=NC2=C(S1)C=C(OC(F)(F)F)C=C2
Relative Density.	1.572 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 240.00 mg/mL (1024.77 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 43.00 mg/mL (183.61 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5.00 mg/mL (21.35 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.2699 mL	21.3495 mL	42.6989 mL	213.4946 mL
5 mM	0.8540 mL	4.2699 mL	8.5398 mL	42.6989 mL
10 mM	0.4270 mL	2.1349 mL	4.2699 mL	21.3495 mL
20 mM	0.2135 mL	1.0675 mL	2.1349 mL	10.6747 mL
50 mM	0.0854 mL	0.4270 mL	0.8540 mL	4.2699 mL
100 mM	0.0427 mL	0.2135 mL	0.4270 mL	2.1349 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.