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Riluzole HCl (RP-54274, PK 26124)

Cat No.:V29099 Purity: ≥98%
Riluzole HCl is an anticonvulsant (antiepileptic/antiseizure) active molecule belonging to the family of use-dependent sodium channel blockers that also inhibits GABA uptake with IC50 of 43 μM.
Riluzole HCl (RP-54274, PK 26124)
Riluzole HCl (RP-54274, PK 26124) Chemical Structure CAS No.: 850608-87-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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50mg
100mg
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Other Forms of Riluzole HCl (RP-54274, PK 26124):

  • Riluzole (RP-54274, PK 26124)
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Riluzole HCl is an anticonvulsant (antiepileptic/antiseizure) active molecule belonging to the family of use-dependent sodium channel blockers that also inhibits GABA uptake with IC50 of 43 μM.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Riluzole hydrochloride is an anticonvulsant medication that falls under the class of use-dependent Na+ channel blockers. It has an IC50 of 43 μM for inhibiting GABA content. Riluzole hydrochloride consistently extended IPSCs but only marginally reduced autologous IPSCs at 20 μM. Furthermore, a substantial, concentration-dependent, and readily reversible increase of the reaction to 2 μM GABA was observed with riluzole hydrochloride. GABA currents exhibited a notable desensitization to 2 μM GABA and riluzole HCl after a sustained co-exposure at higher concentrations, particularly 300 μM. About 60 μM is the EC50 of riluzole hydrochloride for increasing GABA responsiveness [1].
ln Vivo
Systemic injection of riluzole hydrochloride (8 mg/kg, i.p.; n = 6 corresponding) is the standard procedure. In the same group, the duration of ultrasonic induction of vocalizations was longer overall (P<0.05) than the drug-loaded test, although the duration of no vocalizations for one week was lower. When compared to before and after preparation, the systemic treatment of riluzole hydrochloride (8 mg/kg, ip; n = 19 components) dramatically decreased arthritic vocalizations (P <0.05 ~ 0.001).The duration of hearing and ultrasonic vocalizations brought on by fish stimulation is greatly shortened by riluzole hydrochloride.
References

[1]. Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function. Neuropharmacology. 2002 Feb;42(2):199-209.

[2]. Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available riluzole in a rat model of arthritis pain. Mol Pain. 2015 Aug 28;11:51.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C8H6CLF3N2OS
Molecular Weight
270.659249782562
Exact Mass
269.984
CAS #
850608-87-6
Related CAS #
Riluzole;1744-22-5
PubChem CID
6419992
Appearance
White to off-white solid powder
LogP
4.16
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
1
Heavy Atom Count
16
Complexity
238
Defined Atom Stereocenter Count
0
InChi Key
QEAOELIJQRYJJS-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H5F3N2OS.ClH/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5;/h1-3H,(H2,12,13);1H
Chemical Name
6-(trifluoromethoxy)-1,3-benzothiazol-2-amine;hydrochloride
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~369.47 mM)
H2O : ~4.17 mg/mL (~15.41 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (9.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (9.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • Enter 5 in the Volume box and choose the correct unit (mL)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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