| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Flibanserin (BIMT-17; BIMT-17BS; EBD-6396; Girosa; trade name Addyi) is a novel and potent agonist of the 5-HT1A and serotonergic antidepressant approved for the treatment of pre-menopausal women with hypoactive sexual desire disorder (HSDD). The medication increases the number of satisfying sexual events per month by about one half over placebo from a starting point of about two to three.
| ln Vitro |
After oxidative breakdown, flibanserin (0.01-100 μM; 72 h) can be broken down into two potentially non-toxic degradation products, DP1 and DP2 [1]. Determination of cell viability [1]
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| ln Vivo |
In the hippocampus, midbrain, and prefrontal cortex, flibanserin (1, 10, 30 mg/kg; i.p.; single dosage) has unique pharmacological characteristics. The cortex may be more responsive than other brain regions because 5-HT1A receptors are found there [2]. The mesolimbic dopaminergic system and the hypothalamic structures involved in integrating sexual cues associated to sexual motivation are preferentially activated by flibanserin (15, 45 mg/kg; oral; twice daily; 22 days)[3]. Flibanserin (5, 10, 25, and 50 mg/kg; subcutaneous injection; single dosage) reduces anxiety without causing adverse motor effects in a rat ultrasonic vocalization paradigm [4].
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| Cell Assay |
Cell viability determination [1]
Cell Types: NHSF cell lin Tested Concentrations: 0.01, 0.1, 1, 10, 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Cell viability reached 97.91% (DP1) and 96.73% (DP2) at 0.01 μM. Non-toxic at concentrations up to 100 μM (IC50 >100 μM). |
| Animal Protocol |
Animal/Disease Models: Long Evans female rat (225-250 g) [3]
Doses: 15 mg/kg; 45 mg/kg Route of Administration: po (oral gavage); twice (two times) daily for 22 days Experimental Results: Ventral tegmental area The density of activated catecholaminergic neurons increased, but not in the locus coeruleus. After long-term 22-day treatment, Fos expression increased in the medial preoptic area and arcuate nucleus of the hypothalamus, ventral tegmental area, locus coeruleus, and lateral paragigantocellular nucleus. Animal/Disease Models: Infant rat anxiety ultrasonic vocalization model [4] Doses: 5, 10, 25 and 50 mg/kg Route of Administration: subcutaneous injection Experimental Results: Ultrasonic vocalization of infant mice diminished. Shown to be effective within 30 minutes, with no serious motor side effects at active doses. |
| References |
[1]. Fayed M, et al. Insights into Flibanserin Oxidative Stress Degradation Pathway: In Silico – In Vitro Toxicity Assessment of Its Degradates[J]. New Journal of Chemistry, 2021.
[2]. Invernizzi RW, et al. A potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors. Br J Pharmacol. 2003 Aug;139(7):1281-8. [3]. Gelez H, et al. Brain neuronal activation induced by flibanserin treatment in female rats. Psychopharmacology (Berl). 2013 Dec;230(4):639-52. [4]. Podhorna J, et al. Flibanserin has anxiolytic effects without locomotor side effects in the infant rat ultrasonic vocalization model of anxiety. Br J Pharmacol. 2000 Jun;130(4):739-46. [5]. Gelman F, et al. Flibanserin for hypoactive sexual desire disorder: place in therapy. Ther Adv Chronic Dis. 2017 Jan;8(1):16-25. |
| Molecular Formula |
C20H21F3N4O
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|---|---|
| Molecular Weight |
390.41
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| Exact Mass |
390.16675
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| CAS # |
167933-07-5
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| Related CAS # |
Flibanserin-d4-1;2122830-91-3;Flibanserin hydrochloride;147359-76-0;Flibanserin-d4;2122830-90-2
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| SMILES |
FC(C1C([H])=C([H])C([H])=C(C=1[H])N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])N2C(N([H])C3=C([H])C([H])=C([H])C([H])=C23)=O)C([H])([H])C1([H])[H])(F)F
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| Synonyms |
BIMT 17; BIMT 17BS; EBD 6396; BIMT17; BIMT17BS; EBD-6396; BIMT-17; BIMT-17BS; EBD6396; Flibanserin. trade name: Addyi;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~128.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 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 (6.40 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 | 2.5614 mL | 12.8070 mL | 25.6141 mL | |
| 5 mM | 0.5123 mL | 2.5614 mL | 5.1228 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5614 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.
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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