[CAS NO. 850608-87-6] Riluzolehydrochloride

Name: Riluzolehydrochloride
Brand: Arctom Scientific
SKU: HY-B0211A

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PRODUCTS SPECIFICATIONS [850608-87-6]

Store

Catalog

HY-B0211A

Brand

MCE

CAS

850608-87-6

DESCRIPTION [850608-87-6]

Overview

MDL	MFCD02262214
Molecular Weight	270.66
Molecular Formula	C8H6ClF3N2OS
SMILES	NC1=NC2=CC=C(OC(F)(F)F)C=C2S1.Cl

For research use only. We do not sell to patients.

5 Publications Citing Use of MCE

Summary

Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na ⁺ channel blocker which can also inhibit GABA uptake with an IC ₅₀ of 43 μM.

IC50 & Target

Sodium channel ^[1]
IC50: 43 μM (GABA receptor) ^[1]

In Vitro

Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na ⁺ channel blocker which can also inhibit GABA uptake with an IC ₅₀ of 43 μM. At 20 μM, Riluzole hydrochloride inhibits peak autaptic IPSCs only slightly but prolongs IPSCs reliably. It is also found that Riluzole hydrochloride causes a strong, concentration-dependent, readily reversible enhancement of responses to 2 μM GABA. At higher concentrations of Riluzole hydrochloride, especially 300 μM, GABA currents exhibit apparent desensitization during prolonged co-exposure to 2 μM GABA and Riluzole hydrochloride. The EC ₅₀ of Riluzole hydrochloride potentiation of GABA responses is about 60 μM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In normal naïve rats, systemic injection of Riluzole hydrochloride (8 mg/kg, i.p.; n=6 rats) decreases the duration of ultrasonic but not audible vocalizations evoked by noxious stimulation of the knee joint compare to vehicle tested in the same rats (P<0.05). Systemic application of Riluzole hydrochloride (8 mg/kg, i.p.; n=19 rats) decreases the vocalizations of arthritic rats compare to predrug and vehicle significantly (P<0.05 to 0.001). Riluzole hydrochloride administered into the CeA significantly decreases the duration of audible and ultrasonic vocalizations evoked by noxious stimulation of the knee compare to predrug values (n=8 rats; P<0.05 to 0.01) ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01303341	National Cancer Institute (NCI)	Advanced Malignant Solid Neoplasm\|Recurrent Melanoma\|Refractory Malignant Solid Neoplasm\|Stage III Cutaneous Melanoma AJCC v7\|Stage IIIA Cutaneous Melanoma AJCC v7\|Stage IIIB Cutaneous Melanoma AJCC v7\|Stage IIIC Cutaneous Melanoma AJCC v7\|Stage IV Cutaneous Melanoma AJCC v6 and v7	February 18, 2011	Phase 1
NCT00895752	Indiana University\|Indiana Clinical and Translational Sciences Institute	Fragile X Syndrome	April 2009	Phase 4
NCT00353665	University of Lisbon\|H. Lundbeck A+S	Amyotrophic Lateral Sclerosis	July 2005	Phase 2\|Phase 3
NCT03722680	UNICANCER	Oxaliplatin-induced Peripheral Neuropathy	October 28, 2020	Phase 2
NCT04454840	Peking University Third Hospital	Amyotrophic Lateral Sclerosis	May 1, 2016	Early Phase 1
NCT01910259	University College, London\|Medical Research Council\|National Institute for Health Research, United Kingdom\|MS Society\|University of Edinburgh\|Queen Mary University of London\|Keele University\|University of Sheffield\|University of Leeds\|University of Warwick	Secondary Progressive Multiple Sclerosis	December 18, 2014	Phase 2
NCT03127267	AB Science	Amyotrophic Lateral Sclerosis	February 2, 2021	Phase 3
NCT00251303	National Institute of Mental Health (NIMH)\|National Institutes of Health Clinical Center (CC)	Obsessive-Compulsive Disorder\|Autism Spectrum Disorder\|Autism\|Asperger Disorder\|Developmental Disorder	August 2005	Phase 2
NCT02796755	Emory University	Inflammation\|Fatigue	April 2016	Phase 4
NCT03679975	Aquestive Therapeutics\|inVentiv Health Clinical\|Covance	Amyotrophic Lateral Sclerosis	April 4, 2018	Phase 2
NCT04761614	Ning Jin\|Ohio State University Comprehensive Cancer Center	Metastatic Colorectal Carcinoma\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	April 2, 2021	Phase 1
NCT00211224	King´s College London\|Assistance Publique - Hôpitaux de Paris\|University of Ulm\|Aventis Pharmaceuticals	Multiple System Atrophy\|Progressive Supranuclear Palsy	April 2000	Phase 3
NCT01486849	Cytokinetics	Amyotrophic Lateral Sclerosis	November 2011	Phase 2
NCT00542412	Sanofi	Amyotrophic Lateral Sclerosis	January 2001	Phase 4
NCT00805493	National Institute of Mental Health (NIMH)\|National Institutes of Health Clinical Center (CC)	Bipolar Disorder\|Anxiety Disorders\|Bipolar Affective Disorder\|Bipolar Depression	November 2008	Phase 2
NCT02081027	Children´s Hospital Medical Center, Cincinnati	Autism Spectrum Disorders	September 19, 2013	Early Phase 1
NCT01104649	S. Andrea Hospital\|Agenzia Italiana del Farmaco	Cerebellar Ataxia	April 2010	Phase 2\|Phase 3
NCT04745299	Corestem, Inc.	Amyotrophic Lateral Sclerosis	March 23, 2021	Phase 3
NCT00523718	Yale University\|National Institute of Mental Health (NIMH)	Obsessive-compulsive Disorder\|Ocd	September 2006	Phase 2
NCT02238626	MediciNova\|Wake Forest University Health Sciences	Amyotrophic Lateral Sclerosis	September 2014	Phase 2
NCT00026052	National Institute of Mental Health (NIMH)\|National Institutes of Health Clinical Center (CC)	Depression	November 2001	Phase 2
NCT05508074	InFlectis BioScience	Amyotrophic Lateral Sclerosis\|ALS	September 2022	Phase 2
NCT03537807	Biohaven Pharmaceuticals, Inc.	Amyotrophic Lateral Sclerosis\|ALS\|Lou Gehrig Disease\|Lou Gehrig´s Disease\|Lou-Gehrigs Disease\|Motor Neuron Disease, Amyotrophic Lateral Sclerosis
NCT01709149	Cytokinetics	Amyotrophic Lateral Sclerosis	October 2012	Phase 2
NCT00419003	Baylor College of Medicine\|National Alliance for Research on Schizophrenia and Depression\|National Center for Research Resources (NCRR)	Major Depression	December 2006	Phase 4
NCT02859792	Assistance Publique Hopitaux De Marseille	Spinal Cord Injury	May 2019	Phase 2
NCT01257828	AOSpine North America Research Network	Cervical Spondylotic Myelopathy	March 2012	Phase 3
NCT04630444	Mclean Hospital\|Brain & Behavior Research Foundation	Posttraumatic Stress Disorder	March 16, 2017	Early Phase 1
NCT00202397	S. Andrea Hospital	Hereditary Ataxia\|Multiple Sclerosis\|Cerebellar Ataxia	June 2005	Phase 2
NCT01204918	Yale University	Depression	June 2011	Phase 2
NCT02136823	Shirley Ryan AbilityLab	Chronic Spinal Cord Injury	June 2009	Not Applicable
NCT00283309	University of Texas Southwestern Medical Center	Mood\|Memory Deficit	November 2005	Phase 4
NCT03039673	Centre Hospitalier Universitaire de N?mes	Amyotrophic Lateral Sclerosis	June 19, 2017	Phase 2
NCT00277602	Sanofi	Huntington Disease	November 1999	Phase 3
NCT01597518	AOSpine North America Research Network\|AO Foundation, AO Spine\|United States Department of Defense\|Rick Hansen Institute\|Christopher Reeve Paralysis Foundation	Spinal Cord Injury	October 2013	Phase 2\|Phase 3
NCT04950933	Peking University Third Hospital\|The Second Hospital of Hebei Medical University	Amyotrophic Lateral Sclerosis	June 1, 2020	Phase 2\|Phase 3
NCT03347344	Assistance Publique - Hôpitaux de Paris	Spinocerebellar Ataxia Type 2	January 17, 2018	Phase 3
NCT01378676	Cytokinetics	Amyotrophic Lateral Sclerosis	June 2011	Phase 2
NCT04326283	Genuv Inc.	Amyotrophic Lateral Sclerosis	April 2, 2020	Phase 1\|Phase 2
NCT00544544	Mclean Hospital	Bipolar Depression	June 2007	Not Applicable
NCT01703039	Brigham and Women´s Hospital	Major Depressive Disorder	January 2013	Phase 2
NCT00501943	University of California, San Francisco\|National Multiple Sclerosis Society\|Oregon Health and Science University	Multiple Sclerosis	July 2006	Phase 2
NCT00375050	Yale University\|Stanley Medical Research Institute	Schizophrenia\|Schizoaffective	May 2002	Not Applicable
NCT02588677	AB Science	Amyotrophic Lateral Sclerosis (ALS)	April 2013	Phase 2\|Phase 3
NCT00818389	Massachusetts General Hospital\|ALS Association\|ALS Society of Canada\|National Institute of Neurological Disorders and Stroke (NINDS)\|University of Toronto\|State University of New York - Upstate Medical University\|Columbia University\|University of Kentucky	Amyotrophic Lateral Sclerosis	January 2009	Phase 2\|Phase 3
NCT01018056	Johns Hopkins University\|National Institute of Mental Health (NIMH)	Tourette Syndrome	November 2009	Phase 4
NCT05292209	University of Utah\|Ohio State University	Atrial Fibrillation Paroxysmal	June 15, 2022	Phase 2
NCT00376220	Johns Hopkins University\|Stanley Medical Research Institute	Bipolar Disorder	May 2004	Phase 2
NCT03457753	Aquestive Therapeutics\|Inventiv Health\|Covance	ALS	March 1, 2018	Phase 2
NCT01661855	Evdokia Anagnostou\|Holland Bloorview Kids Rehabilitation Hospital\|McMaster University\|The Hospital for Sick Children\|University of Western Ontario, Canada\|Unity Health Toronto\|University of Toronto\|Anagnostou, Evdokia, M.D.	Autism Spectrum Disorders	September 2013	Phase 2
NCT00876889	The Methodist Hospital Research Institute\|Christopher Reeve Paralysis Foundation\|United States Department of Defense\|AO Clinical Investigation and Publishing Documentation\|Ontario Neurotrauma Foundation	Spinal Cord Injury	April 2010
NCT00054704	National Institute of Mental Health (NIMH)\|National Institutes of Health Clinical Center (CC)	Bipolar Disorder	February 2003	Phase 2
NCT00866840	Rutgers, The State University of New Jersey\|National Cancer Institute (NCI)	Melanoma (Skin)	April 2009	Phase 2
NCT04819438	Cross Research S.A.\|Zambon SpA	Bioequivalence	January 15, 2021	Phase 1
NCT03660917	S. Andrea Hospital	SCA7	January 1, 2019	Phase 2\|Phase 3
NCT01703117	Icahn School of Medicine at Mount Sinai\|Rockefeller University	Alzheimer´s Disease	November 2013	Phase 2
NCT02019940	Yale University\|National Center for PTSD	PTSD	January 2014	Phase 1
NCT00667901	University of Medicine and Dentistry of New Jersey\|National Cancer Institute (NCI)\|Rutgers, The State University of New Jersey	Melanoma (Skin)	February 2007	Phase 1
NCT01018836	Rutgers, The State University of New Jersey\|National Cancer Institute (NCI)	Metastatic Cancer\|Unspecified Adult Solid Tumor, Protocol Specific	November 2009	Phase 1
NCT02155829	Uniformed Services University of the Health Sciences\|U.S. Army Medical Research and Development Command	PTSD	July 2013	Phase 1\|Phase 2
NCT00868166	Hoffmann-La Roche\|European Commission	Amyotrophic Lateral Sclerosis	April 30, 2009	Phase 3
NCT02645461	University of Roma La Sapienza	Amyotrophic Lateral Sclerosis	January 2014	Not Applicable
NCT00774423	Assistance Publique - Hôpitaux de Paris	SMA	January 2006	Phase 2\|Phase 3
NCT03272802	Isfahan University of Medical Sciences	Neuromuscular Diseases	March 16, 2017	Phase 2\|Phase 3
NCT00903214	Barbara Ann Karmanos Cancer Institute\|National Cancer Institute (NCI)	Breast Cancer	May 2009	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 369.47 mM ; Need ultrasonic)

H ₂ O : 4.17 mg/mL ( 15.41 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6947 mL	18.4734 mL	36.9467 mL
5 mM	0.7389 mL	3.6947 mL	7.3893 mL
10 mM	0.3695 mL	1.8473 mL	3.6947 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (9.24 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (9.24 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (9.24 mM); Clear solution

* All of the co-solvents are available by MCE.