Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Riluzole [1744-22-5]

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Referência T0349-1ml

Tamanho : 1mLx10mM(inDMSO)

Marca : TargetMol

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Riluzole

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

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.

Batch Information

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Purity:99.88%

Color:White to Yellow

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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.