2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Flibanserin

Flibanserin  (Synonyms: BIMT-17; BIMT-17BS)

Cat. No.: HY-A0095 Purity: 99.54%
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Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research-.

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

Flibanserin Chemical Structure

Flibanserin Chemical Structure

CAS No. : 167933-07-5

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Based on 2 publication(s) in Google Scholar

Other Forms of Flibanserin:

Flibanserin Related Antibodies

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research[1]-[5].

IC50 & Target[2]

5-HT1A Receptor

1 nM (Ki)

5-HT2A Receptor

49 nM (Ki)

dopamine D4 receptors

4-24 nM (Ki)

In Vitro

Flibanserin (0.01-100 μM; 72 h) can transform into two degradation products DP1 and DP2 with no toxicity potential after oxidative degradation[1].

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

Flibanserin Related Antibodies

Cell Viability Assay[1]

Cell Line: NHSF cell lin
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Resulted cell viability reached to 97.91% (DP1) and 96.73% (DP2) at 0.01 μM.
Showed non-toxic up to 100 μM (IC50 >100 μM).
In Vivo

Flibanserin (1, 10, 30 mg/kg; i.p.; single dose) shows different pharmacological properties in prefrontal cortex, hippocampus and midbrain. The 5-HT1A receptor occupancy in cortex indicates it’s the more sensitive than other brain region[2].
Flibanserin (15, 45 mg/kg; p.o.; twice a day; 22 d) preferentially activates the brain regions belonging to the mesolimbic dopaminergic pathway and hypothalamic structures involved in the integration of sexual cues related to sexual motivation[3].
Flibanserin (5, 10, 25, and 50 mg/kg; s.c.; single dose) has anxiolytic effects without locomotor side effects in rat ultrasonic vocalization model[4].

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

Animal Model: Long Evans female rats (225-250 g)[3]
Dosage: 15 mg/kg; 45 mg/kg
Administration: Oral gavage; twice a day for 22 days
Result: Increased the density of activated catecholaminergic neurons in the ventral tegmental area but not in the locus coeruleus.
Increased Fos expression in the medial preoptic area and arcuate nucleus of the hypothalamus, ventral tegmental area, locus coeruleus, and lateral paragigantocellular nucleus with chronic 22-day treatment.
Animal Model: Rat pup ultrasonic vocalization model of anxiety[4]
Dosage: 5, 10, 25, and 50 mg/kg
Administration: Subcutaneous injection
Result: Reduced ultrasonic vocalizations in rat pups.
Showed effective within 30 min and has no severe locomotor side effects at active doses.
Clinical Trial
Molecular Weight

390.40

Formula

C20H21F3N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=CC=CC=C2N1CCN3CCN(C4=CC=CC(C(F)(F)F)=C4)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (128.07 mM; Need ultrasonic; 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 2.5615 mL 12.8074 mL 25.6148 mL
5 mM 0.5123 mL 2.5615 mL 5.1230 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • 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 (6.40 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 (6.40 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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5615 mL 12.8074 mL 25.6148 mL 64.0369 mL
5 mM 0.5123 mL 2.5615 mL 5.1230 mL 12.8074 mL
10 mM 0.2561 mL 1.2807 mL 2.5615 mL 6.4037 mL
15 mM 0.1708 mL 0.8538 mL 1.7077 mL 4.2691 mL
20 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2018 mL
25 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5615 mL
30 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1346 mL
40 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
50 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2807 mL
60 mM 0.0427 mL 0.2135 mL 0.4269 mL 1.0673 mL
80 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8005 mL
100 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6404 mL
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Flibanserin Related Classifications

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.

Keywords:

Flibanserin167933-07-5BIMT-17 BIMT-17BSBIMT17BIMT 175-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptoraffinityneurotransmitterhypoactivesexualdesiredisorderantidepressantantianxietyhypoactive sexual desire disorderHSDDorally activeDP1DP2no cytotoxicityNHSF cell lineprefrontal cortexhippocampusmidbrainInhibitorinhibitorinhibit

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