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Pitolisant hydrochloride

Catalog No. T7176 CAS 903576-44-3

Synonyms: BF 2649, Ciproxidine

Pitolisant hydrochloride (Ciproxidine) is a potent and selective inverse agonist of the histamine H3 receptor(Ki : 0.16 nM).

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Pitolisant hydrochloride Chemical Structure

Pitolisant hydrochloride, CAS 903576-44-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 328.00
200 mg	In stock	$ 492.00
500 mg	In stock	$ 787.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.72%

Purity: 99.26%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pitolisant hydrochloride (Ciproxidine) is a potent and selective inverse agonist of the histamine H3 receptor(Ki : 0.16 nM).
Targets&IC50	H3 receptor:0.16 nM(ki)
In vivo	Mice fed with high-fat diet showed more weight gain throughout the 12-week period of inducing obesity. Animals fed with high-fat diet and treated with pitolisant (next 14 days) showed significantly less weight gain than mice from the control group consuming a high-fat diet. From the 10th day of the pitolisant administration, a statistically significant difference in body weight between the groups was observed. Metformin, which served as a positive control, reduced body weight from the ninth day of administration onward[1].
Animal Research	Male CD-1 mice were fed on high-fat diet consisting of 40% fat blend (Labofeed B with 40% lard) for 14 weeks, water and 30% sucrose available ad libitum. Control mice were fed on a standard diet and drank water only. After 12 weeks, mice with obesity induced via their diet were randomly divided into three equal groups that had the same mean body weight and were treated intraperitoneally with test compounds at the following doses: pitolisant 10 mg/kg bw/day or metformin 100 mg/kg bw/day; control group: vehicle =1% Tween 80, 0.35 ml/kg (high-fat/sugar diet + vehicle = obesity control group) once daily in the morning, between 9:00 and 10:00 AM for 14 days. Control mice (control without obesity) were maintained on a standard diet, with intraperitoneal administration of vehicle = 1% Tween 80, 0.35 ml/kg (standard diet + vehicle = control group). Water and sucrose were measured daily, immediately prior to administration of drugs. Animals always had free access to feed, water and sucrose[1].

Synonyms	BF 2649, Ciproxidine
Molecular Weight	332.31
Formula	C17H27Cl2NO
CAS No.	903576-44-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 43 mg/mL (129.40 mM)

References and Literature

1. Kotańska Magdalena, Kuder K J , Szczepańska Katarzyna, et al. The histamine H3 receptor inverse agonist pitolisant reduces body weight in obese mice[J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 2018. 2. Schwartz J C . The histamine H3 receptor: from discovery to clinical trials with pitolisant[J]. British journal of pharmacology, 2011, 163(4):713-721.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Drug Library GPCR Compound Library FDA-Approved & Pharmacopeia Drug Library Histamine & Melatonin Receptor-Targeted Compound Library

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

Pitolisant hydrochloride 903576-44-3 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor BF2649 inhibit Pitolisant Hydrochloride Inhibitor BF 2649 Ciproxidine Pitolisant BF-2649 inhibitor

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