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Pitolisant hydrochloride

Name: Pitolisant hydrochloride
Brand: Selleck Chemicals
SKU: S5926
Rating: 5 (1 reviews)

Synonyms: Tiprolisant hydrochloride, BF-2649 HCl

Catalog No.S5926 Purity: 99.96%

Pitolisant (Tiprolisant, BF-2649) acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype.

Pitolisant hydrochloride Chemical Structure

CAS: 903576-44-3

Purity & Quality Control

Batch: S592601 DMSO] 66 mg/mL] false] Water] 66 mg/mL] false] Ethanol] 66 mg/mL] false Purity: 99.96%

99.96

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Signaling Pathway

Histamine Receptor Signaling Pathway

Choose Selective Histamine Receptor Inhibitors

Biological Activity

Description

Pitolisant (Tiprolisant, BF-2649) acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype.

Targets

H3 receptor ^[1]

0.16 nM(Ki)

In vitro
In vitro	Pitolisant shows high selectivity for H3 receptors compared with the other histamine receptor subtypes (H1, H2, and H4 subtypes) and shows a lack of interaction with other human receptors or channels^[1].

In Vivo
In vivo	In animal experiments, pitolisant increases histaminergic and noradrenergic neuron activity, increases wakefulness at the expense of slow wave and rapid eye movement sleep, has low abuse potential, and has no effect on mechanical or thermal pain thresholds^[1].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05458128	Active not recruiting	Idiopathic Hypersomnia\|Excessive Daytime Sleepiness	Harmony Biosciences LLC	August 19 2022	Phase 3
NCT02929342	Completed	Healthy Volunteers	Bioprojet	July 2016	Phase 1
NCT02611687	Active not recruiting	Narcolepsy With Cataplexy\|Narcolepsy Without Cataplexy	Bioprojet	June 6 2016	Phase 3

References

[1] Calik MW. Nat Sci Sleep. 2017, 9:127-133.

Chemical Information & Solubility

Molecular Weight	332.31	Formula	C₁₇H₂₇Cl₂NO
CAS No.	903576-44-3	SDF	--
Smiles	C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl.Cl
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 66 mg/mL ( (198.6 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 66 mg/mL

Ethanol : 66 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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