1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Sodium Channel
    GABA Receptor

Riluzole hydrochloride (Synonyms: PK 26124 hydrochloride)

Cat. No.: HY-B0211A Purity: 99.94%
Handling Instructions

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 IC50 of 43 μM.

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

Riluzole hydrochloride Chemical Structure

Riluzole hydrochloride Chemical Structure

CAS No. : 850608-87-6

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10 mM * 1 mL in Water USD 55 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
100 mg USD 72 In-stock
Estimated Time of Arrival: December 31
500 mg USD 140 In-stock
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Other Forms of Riluzole hydrochloride:

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  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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 IC50 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 IC50 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 EC50 of Riluzole hydrochloride potentiation of GABA responses is about 60 μM[1].

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

H2O : 131 mg/mL (484.00 mM; Need ultrasonic and warming)

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.
References
Cell Assay
[1]

Two-electrode voltage clamp of Xenopus oocytes expressing exogenous GABAA receptors is performed with a CA-1B high performance oocyte clamp. The extracellular recording solution is ND-96 medium. Riluzole hydrochloride is applied from a common tip via a gravity-driven multibarrel drug-delivery system. Data acquisition and analysis are performed with pCLAMP 6 software[1].

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

Animal Administration
[2]

Adult male Sprague-Dawley rats (180 to 350 g) are housed in a temperature-controlled room and maintained on a 12-h day/night cycle with unrestricted access to food and water. Pain behaviors are measured before and 5 h after induction of a mono-arthritis in the left knee joint. To test the effects of systemic (intraperitoneal, i.p.) application of Riluzole hydrochloride, pain behaviors are measured 1 h postinjection of Riluzole hydrochloride in normal and arthritic animals. To determine effects of Riluzole hydrochloride into the amygdala, pain behaviors are measured 15 min after starting Riluzole hydrochloride application through a stereotaxically implanted microdialysis probe. To investigate site of action in the amygdala of systemically applied Riluzole hydrochloride, potassium channel blockers are administered into the amygdala 45 min after systemic application of Riluzole hydrochloride and pain behaviors are measured 15 min later, i.e., 1 h postinjection of riluzole (i.p.)[2].

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

References
Molecular Weight

270.66

Formula

C₈H₆ClF₃N₂OS

CAS No.

850608-87-6

SMILES

NC1=NC2=CC=C(OC(F)(F)F)C=C2S1.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Riluzole hydrochloride
Cat. No.:
HY-B0211A
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Riluzole hydrochloride

Cat. No.: HY-B0211A