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IPSU

Catalog No. T5503 CAS 1373765-19-5

IPSU is an antagonist of OX2 receptor. IPSU Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors.

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IPSU, CAS 1373765-19-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 57.00
2 mg	In stock	$ 82.00
5 mg	In stock	$ 131.00
10 mg	In stock	$ 168.00
25 mg	In stock	$ 353.00
50 mg	In stock	$ 526.00
100 mg	In stock	$ 759.00
1 mL * 10 mM (in DMSO)	In stock	$ 141.00

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Purity: 98.1%

Biological Description

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Description	IPSU is an antagonist of OX2 receptor. IPSU Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors.
Targets&IC50	OX2:7.85 (pKi) , OX1:6.29 (pKi)
In vitro	BBAC or the selective OX2R antagonist IPSU bind rapidly and reach equilibrium very quickly in binding and/or functional assays[1].
In vivo	IPSU?exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration.?IPSU increases sleep when dosed during the mouse active phase (lights off);?IPSU induces sleep primarily by increasing NREM sleep.?IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing.?The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day[2]

Molecular Weight	405.49
Formula	C23H27N5O2
CAS No.	1373765-19-5

Storage

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

Solubility Information

DMSO: 30 mg/mL (73.98 mM)

References and Literature

1. Callander GE, et al. Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors. Front Neurosci. 2013 Dec 3;7:230. 2. Betschart C, et al. Identification of a novel series of orexin receptor antagonists with a distinct effect on sleeparchitecture for the treatment of insomnia. J Med Chem. 2013 Oct 10;56(19):7590-607.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Bioactive Compound Library NO PAINS Compound Library Orally Active 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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

IPSU 1373765-19-5 GPCR/G Protein Neuroscience OX Receptor inhibit HCRT Receptor Hypocretin Receptor Orexin Receptor (OX Receptor) Inhibitor inhibitor

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