2. GPCR/G Protein
    Neuronal Signaling
  3. Neurokinin Receptor
  4. Eprazinone dihydrochloride

Eprazinone dihydrochloride 

Cat. No.: HY-B2078A Purity: ≥98.0%
COA Handling Instructions

Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen.

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

Eprazinone dihydrochloride Chemical Structure

Eprazinone dihydrochloride Chemical Structure

CAS No. : 10402-53-6

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10 mM * 1 mL in DMSO USD 94 In-stock
Estimated Time of Arrival: December 31
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100 mg USD 140 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen[1][2].

IC50 & Target

Neurokinin 1 receptor[1]
In Vitro

Eprazinone specifically displaces binding to the NK1R. Although Eprazinone displays a rather weak inhibition of [125I]BH-SP binding to NK1R, at a concentration of 25 μM, and an antagonistic effect of about 30%, NK1R blockade could contribute to its mucolytic activity[2].

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

Eprazinone (50-200 mg/kg; oral gavage; daily; for 4 days; adult male rats) at a dose of 200 mg/kg significantly increases total and individual (with the exception of phosphatidylinositol) phospholipid levels and decreases total neutral lipids. Lower doses of Eprazinone significantly decrease neutral lipid levels without affecting the phospholipids[1].
In airway epithelial studies, mucosal addition of Eprazinone produces a dose-dependent partially reversible decrease in short-circuit current (Isc). The decrease in Isc at lower Eprazinone concentrations is accounted for entirely by a decrease in net chloride secretion while at higher concentrations both sodium and chloride transport are affected[1].

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

Animal Model: Adult male pathogen free Fischer 344 inbred rats (200-250 g)[1]
Dosage: 50 mg/kg, 100 mg/kg, and 200 mg/kg
Administration: Oral gavage; daily; for 4 days
Result: At a dose of 200 mg/kg significantly increased total and individual (with the exception of phosphatidylinositol) phospholipid levels and decreased total neutral lipids.
Molecular Weight

453.44

Appearance

Solid

Formula

C24H34Cl2N2O2
CAS No.
SMILES

O=C(C1=CC=CC=C1)C(C)CN2CCN(CC(OCC)C3=CC=CC=C3)CC2.Cl[H].Cl[H]
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)
Solvent & Solubility
In Vitro: 

H2O : ≥ 25 mg/mL (55.13 mM)

DMSO : 6.25 mg/mL (13.78 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2054 mL 11.0268 mL 22.0536 mL
5 mM 0.4411 mL 2.2054 mL 4.4107 mL
10 mM 0.2205 mL 1.1027 mL 2.2054 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (13.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.62 mg/mL (1.37 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.62 mg/mL (1.37 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Keywords:

Eprazinone10402-53-6Neurokinin ReceptorNK receptorTachykinin receptorPhospholipidpulmonaryarterialpO2chloridetransportmucolyticsecretolyticantispasmodicantitussiveNK1RInhibitorinhibitorinhibit

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