Cat. No.: HY-A0095A

Flibanserin hydrochloride (propan-2-ol) hydrate

(Synonyms: BIMT-17 hydrochloride (propan-2-ol) hydrate; BIMT-17BS hydrochloride (propan-2-ol) hydrate)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

Flibanserin (BIMT-17) hydrochloride (propan-2-ol) hydrate is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with K_i values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride (propan-2-ol) hydrate binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin hydrochloride (propan-2-ol) hydrate 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.

Purity: 99.04%
Formula: C₂₀H₂₂ClF₃N₄O.0.5C₃H₈O.0.5H₂O
Molecular Weight:465.20

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Flibanserin hydrochloride (propan-2-ol) hydrate Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

5-HT_1A Receptor

5-HT_2A Receptor

5-HT_1A Receptor

1 nM (Ki)

5-HT_2A Receptor

49 nM (Ki)

All 5-HT Receptor Isoforms :

In Vitro

Flibanserin (0.01-100 μM; 72 h) hydrochloride (propan-2-ol) hydrate 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.

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) hydrochloride (propan-2-ol) hydrate 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) hydrochloride (propan-2-ol) hydrate 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) hydrochloride (propan-2-ol) hydrate 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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

Appearance Solid
Molecular Weight 465.20
Formula C₂₀H₂₂ClF₃N₄O.0.5C₃H₈O.0.5H₂O
Color White to off-white
SMILES

O=C1NC2=C(N1CCN3CCN(CC3)C4=CC=CC(C(F)(F)F)=C4)C=CC=C2.CC(O)C.Cl.[0.5].O.[0.5]
Synonyms

BIMT-17 hydrochloride (propan-2-ol) hydrate; BIMT-17BS hydrochloride (propan-2-ol) hydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (2)

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Journal Impact Factor

Mol Pharmacol

G α Protein Signaling Bias at Serotonin 1A Receptor. [Abstract]

2023 Nov;104(5):230-238. PMID: 37567783
Authorea

2023 Apr 17.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[3]. Gelez H, et al. Brain neuronal activation induced by flibanserin treatment in female rats. Psychopharmacology (Berl). 2013 Dec;230(4):639-52. [Content Brief]

[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. [Content Brief]

[5]. Gelman F, et al. Flibanserin for hypoactive sexual desire disorder: place in therapy. Ther Adv Chronic Dis. 2017 Jan;8(1):16-25. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Flibanserin hydrochloride (propan-2-ol) hydrate

2 Cited Publications

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Flibanserin hydrochloride (propan-2-ol) hydrate

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Publications Citing Use of MedChemExpress (MCE) Flibanserin hydrochloride (propan-2-ol) hydrate

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Publications (2)

Purity & Documentation

References

Calculators

Help & FAQs

Flibanserin hydrochloride (propan-2-ol) hydrate

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Dopamine Receptor Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Flibanserin hydrochloride (propan-2-ol) hydrate

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Publications (2)

Purity & Documentation

References

Calculators

Help & FAQs

Flibanserin hydrochloride (propan-2-ol) hydrate Related Classifications

HY-A0095A Related Classifications