2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. IPSU

IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

For research use only. We do not sell to patients.

IPSU Chemical Structure

IPSU Chemical Structure

CAS No. : 1373765-19-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 149 In-stock
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10 mM * 1 mL in DMSO USD 149 In-stock
Solid
1 mg USD 34 In-stock
5 mg USD 135 In-stock
10 mg USD 216 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

IPSU Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE IPSU

View All Orexin Receptor (OX Receptor) Isoform Specific Products:

View All Isoforms
OX2 Receptor OX1 Receptor

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

IC50 & Target

pKi: 7.85 (OX2R), 6.29 (OX1R)[1]
In Vitro

Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

IPSU Related Antibodies
In Vivo

IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It 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 [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

405.49

Formula

C23H27N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC=NC(N(CC2)CCC2(C3=O)CCCN3CC4=CNC5=CC=CC=C54)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (73.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4662 mL 12.3308 mL 24.6615 mL
5 mM 0.4932 mL 2.4662 mL 4.9323 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Kinase Assay
[2]

Competition experiments are performed with a single concentration of radioligand and six concentrations of competitor (unlabeled ligands; BBAC, almorexant, SB-649868, suvorexant, filorexant or IPSU). 4.6 nM [3H]-BBAC is added simultaneously with various concentrations of unlabeled ligand (0.1 nM-10 μM) to membranes (150 μL/well) in 50 μL/well of assay buffer with a total volume of 250 μL/well. The amount of [3H]-BBAC bound to receptors is determined at room temperature at different time points (ranging from 15 min to 4 h) and terminated by rapid vacuum filtration and liquid scintillation counting[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Freely moving C57Bl/6 mice with chronically implanted electrodes are well abituated to the experiment boxes and had access to food and ater ad libitum. The test compounds (IPSU) or vehicle are administered per os as a suspension in 0.5% methylcellulose immediately prior to lights off and start of recording. Movement is recorded using infrared sensors in the roof of the box. EEG/EMG signals and motility data are used to score 10 s epochs into wake, NREM sleep, and REM sleep. Each animal served as its own control by application and recording of vehicle the day before compound (IPSU) dosing[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4662 mL 12.3308 mL 24.6615 mL 61.6538 mL
5 mM 0.4932 mL 2.4662 mL 4.9323 mL 12.3308 mL
10 mM 0.2466 mL 1.2331 mL 2.4662 mL 6.1654 mL
15 mM 0.1644 mL 0.8221 mL 1.6441 mL 4.1103 mL
20 mM 0.1233 mL 0.6165 mL 1.2331 mL 3.0827 mL
25 mM 0.0986 mL 0.4932 mL 0.9865 mL 2.4662 mL
30 mM 0.0822 mL 0.4110 mL 0.8221 mL 2.0551 mL
40 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5413 mL
50 mM 0.0493 mL 0.2466 mL 0.4932 mL 1.2331 mL
60 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0276 mL
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IPSU Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IPSU1373765-19-5Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorInhibitorinhibitorinhibit

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