Riluzole (PK 26124) - Moligand™, 10mM in DMSO , Sodium channel alpha subunit blocker, CAS No.1744-22-5, Sodium channel alpha subunit blocker

CAS: 1744-22-5 Cat. No.: R408717 Molecular Weight: 234.2 EC Number: 605-724-6 PubChem CID: 5070

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

RP-54274 | 6-​(trifluoromethoxy)​-2-​benzothiazolamine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
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 Riluzole inhibits currents evoked by N-methyl-D-aspartate (NMDA) (IC50 = 18 μM) and kainic acid (IC50 = 167 μM). Riluzole 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). Riluzole also blocks some of the postsynaptic effects of glutamic acid by noncompetitive blockade of NMDA receptors. Tiluzole 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. Riluzole 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 Riluzole treatment (8 mg/kg i.p.).
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

RP-54274 | 6-​(trifluoromethoxy)​-2-​benzothiazolamine

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ACTIVATOR, BLOCKER, CHANNEL BLOCKER, GATING INHIBITOR

Mechanism of action

Sodium channel alpha subunit blocker

Product Properties

• ALogP: 3.6

Names and Identifiers

• Isomeric SMILES: C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N
• WGK Germany: 3
• RTECS: DL2830000
• PubChem CID: 5070
• Molecular Weight: 234.2

Associated Targets(Human)

CYP1A2 Tchem Cytochrome P450 1A2 (2 Activities)

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SCN2A Tclin Sodium channel protein type 2 subunit alpha (1 Activities)

Discover Target: SCN2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRPC5 Tchem Short transient receptor potential channel 5 (1 Activities)

Discover Target: TRPC5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNN4 Tchem Intermediate conductance calcium-activated potassium channel protein 4 (1 Activities)

Discover Target: KCNN4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCND3 Tclin Potassium voltage-gated channel subfamily D member 3 (1 Activities)

Discover Target: KCND3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNN1 Tchem Small conductance calcium-activated potassium channel protein 1 (1 Activities)

Discover Target: KCNN1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNN3 Tchem Small conductance calcium-activated potassium channel protein 3 (1 Activities)

Discover Target: KCNN3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNN2 Tchem Small conductance calcium-activated potassium channel protein 2 (1 Activities)

Discover Target: KCNN2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Water: 21 mg/mL (72.46 mM); DMSO: 1 mg/mL (3.45 mM); Ethanol: Insoluble
• Melt Point(°C): 118 °C

References

1. Yanan Liu, Guixue Chen, Maojian Li, Man Li, Daoxuan Xie, Zheng Luo.  (2025)  Development of long-acting riluzole transdermal patch against amyotrophic lateral sclerosis: Mechanistic insights into polyglyceryl-3 dioleate-enhanced drug release and skin permeation.  International Journal of Pharmaceutics-X,      [PMID:40735390] [10.1016/j.ijpx.2025.100363]

2. Yu Li, Huimin Niu, Zidan Cao, Zheqi Wang, Jiao Sha, Liukai Zhu, Fengxin Guo, Yuanhui Chong, Tao Li, Baozeng Ren.  (2021)  Equilibrium solubility, model evaluation and molecular dynamic simulation of riluzole in three binary solvents from 278.15 K to 323.15 K.  JOURNAL OF CHEMICAL THERMODYNAMICS,      [PMID:] [10.1016/j.jct.2021.106714]

3. Huimin Niu, Zidan Cao, Xiaoqing Yang, Jiao Sha, Yu Li, Tao Li, Baozeng Ren.  (2021)  The solubility data, Hansen solubility parameter and dissolution thermodynamic properties of riluzole in twelve organic solvents.  JOURNAL OF CHEMICAL THERMODYNAMICS,      [PMID:] [10.1016/j.jct.2021.106569]