Name: Riluzole
Brand: Selleck Chemicals
SKU: S1614
Rating: 5 (13 reviews)

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Control de calidad (Quality Control)

Lote: Pureza: 99.88%

99.88

Dianas relacionadas	CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Otros Sodium Channel Inhibidores	Camostat Mesilate A-803467 cariporide Tolperisone HCl Vinpocetine Veratramine Bulleyaconi cine A GS967 Ambroxol HCl Benzocaine

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	234.2	Fórmula	C₈H₅F₃N₂OS	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	1744-22-5	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	RP-54274, PK 26124			Smiles	C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 47 mg/mL (200.68 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 47 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	4.000mg/ml (17.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	Sodium channel NMDA receptor Glutamate release
In vitro	Riluzole inhibits the release of glutamic acid from cultured neurons, and from brain slices. These effects may be partly due to inactivation of voltage-dependent sodium channels on glutamatergic nerve terminals, as well as activation of a G-protein-dependent signal transduction process. Electrophysiologic experiments performed on isolated excitatory amino acid receptors expressed in the Xenopus oocyte have revealed that this compound inhibits currents evoked by N-methyl-D-aspartate (NMDA) (IC50 = 18 μM) and kainic acid (IC50 = 167 μM). It has been shown to stabilize inactivated sodium channels in frog sciatic nerve, in rat cerebellar granule cells, and on recombinant rat sodium channels expressed in Xenopus oocytes (K_i = 0.2 μM). This chemical also blocks some of the postsynaptic effects of glutamic acid by noncompetitive blockade of NMDA receptors. It protects cultured neurons from anoxic damage, from the toxic effects of glutamic-acid-uptake inhibitors, and from the toxic factor in the CSF of patients with amyotrophic lateral sclerosis.
In vivo	Riluzole can easily cross the blood-brain barrier. This compound has neuroprotective, anticonvulsant, and sedative properties in vivo. In a rodent model of transient global cerebral ischemia, a complete suppression of the ischemia-evoked surge in glutamic acid release has been observed by this chemical treatment (8 mg/kg i.p.).
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/8959995/ [2] http://link.springer.com/article/10.1007%2FPL00005241

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	p-AKT / AKT p-Smad2 / Smad2 / p-Smad3 / Smad3		23077590

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06270108	Recruiting	Treatment-resistant Schizophrenia\|Treatment-responsive Schizophrenia\|Healthy Controls	King''s College London\|South London and Maudsley NHS Foundation Trust	November 14 2022	Early Phase 1
NCT05292209	Recruiting	Atrial Fibrillation Paroxysmal	University of Utah\|Ohio State University	June 15 2022	Phase 2
NCT04819438	Completed	Bioequivalence	Cross Research S.A.\|Zambon SpA	January 15 2021	Phase 1
NCT02859792	Recruiting	Spinal Cord Injury	Assistance Publique Hopitaux De Marseille	May 27 2019	Phase 2
NCT04630444	Completed	Posttraumatic Stress Disorder	Mclean Hospital\|Brain & Behavior Research Foundation	March 16 2017	Early Phase 1

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C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Riluzole Sodium Channel inhibitor

Estructura química

Peso molecular: 234.2