1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Fluspirilene

Fluspirilene  (Synonyms: R 6218; Redeptin)

Cat. No.: HY-B1655 Purity: ≥98.0%
SDS COA Handling Instructions

Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic agent used for schizophrenia.

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

Fluspirilene Chemical Structure

Fluspirilene Chemical Structure

CAS No. : 1841-19-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 105 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 150 In-stock
25 mg USD 270 In-stock
50 mg USD 405 In-stock
100 mg USD 610 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Fluspirilene

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic agent used for schizophrenia.

IC50 & Target

L-type calcium channel

 

Cellular Effect
Cell Line Type Value Description References
H4 EC50
2.4 μM
Compound: 1
Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis
Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis
[PMID: 21126871]
Vero C1008 IC50
3.16 μM
Compound: Fluspirilene
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 CC50
30.33 μM
Compound: Fluspirilene
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 CC50
30.33 μM
Compound: Fluspirilene
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
5.32 μM
Compound: Fluspirilene
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
In Vitro

Fluspirilene, at concentrations which non-competitively modify dihydropyridine binding, selectively antagonizes the effects of calcium-channel activators[1]. Fluspirilene decreases the viability and suppresses sphere-forming of glioma stem cell lines in a dose-dependent manner. Fluspirilene demonstrates the inhibition of proliferation of T98, U87 and all GSC lines at 1.25, 2.5, and 5 μM, while it inhibits the proliferation of U251 and SNB19 at 2.5 and 5 μM[2].

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

In Vivo

Mice treated with Fluspirilene (HY-B1655) shows a remarkable reduction of the tumor size. Fluspirilene significantly prolongs survival of the TGS04 mouse model[2].

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

Clinical Trial
Molecular Weight

475.57

Formula

C29H31F2N3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (52.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1027 mL 10.5137 mL 21.0274 mL
5 mM 0.4205 mL 2.1027 mL 4.2055 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.66%

References
Cell Assay
[2]

To investigate the effect of fluspirilene on cell proliferation, cells are treated with 1.25, 2.5, and 5 μM of fluspirilene. GSC viability is assessed using a Cell Counting Kit-8[2].

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

Animal Administration
[2]

Mice[2]

The mice are randomly assigned to two groups and treated with either fluspirilene (n=5) or with DMSO as a control group (n=5). All mice are given intramuscular injections of 200 μL of DMSO or fluspirilene dissolved in DMSO at 1 mg/kg body weight four times[2].

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1027 mL 10.5137 mL 21.0274 mL 52.5685 mL
5 mM 0.4205 mL 2.1027 mL 4.2055 mL 10.5137 mL
10 mM 0.2103 mL 1.0514 mL 2.1027 mL 5.2568 mL
15 mM 0.1402 mL 0.7009 mL 1.4018 mL 3.5046 mL
20 mM 0.1051 mL 0.5257 mL 1.0514 mL 2.6284 mL
25 mM 0.0841 mL 0.4205 mL 0.8411 mL 2.1027 mL
30 mM 0.0701 mL 0.3505 mL 0.7009 mL 1.7523 mL
40 mM 0.0526 mL 0.2628 mL 0.5257 mL 1.3142 mL
50 mM 0.0421 mL 0.2103 mL 0.4205 mL 1.0514 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Fluspirilene
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HY-B1655
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