country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-14790A

Copy Link Print Information

Esreboxetine succinate

Name: Esreboxetine succinate
Brand: MedChemExpress
SKU: HY-14790A
Availability: PreOrder

(Synonyms: PNU-165442G; (S,S)-Reboxetine succinate)

Esreboxetine succinate (PNU-165442G; (S,S)-Reboxetine succinate) is a selective norepinephrine transporter (NET) inhibitor, with a pIC₅₀ of 9.6 and a pK_i of 9.2 in rats, and it can cross the blood-brain barrier. Esreboxetine succinate increases urethral closure pressure and urethral resistance in rats. Esreboxetine succinate is applicable to research related to inflammatory pain and stress urinary incontinence.

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

CAS No.: 635724-55-9
Formula: C₂₃H₂₉NO₇
Molecular Weight:431.48

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Esreboxetine succinate Chemical Structure

CAS No.: 635724-55-9

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

In Vitro

Esreboxetine (10 pM-100 μM; 6 h) succinate exhibits 20,000-fold higher selectivity for the rat norepinephrine transporter over the serotonin transporter in in vitro radioligand binding assays, with a pK_i of 9.2 for rat NET and 5.6 for rat SERT^[1].
Esreboxetine (10 pM-100 μM; 30 min pre-incubation, 6 min incubation) succinate potently and selectively inhibits norepinephrine uptake in rat cortical synaptosomes, with a pIC₅₀ of 9.6 for rat NET and a pIC₅₀ of 5.3 for rat SERT, representing a 20,000-fold selectivity for NET over SERT^[1].

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

In Vivo

A fixed-dose combination of esreboxetine succinate (10 mg/kg; i.p.; single administration) and Fluoxetine (HY-B0102) (1 mg/kg; i.p.; single administration) enhances the analgesic effect of morphine in the rat formalin model and achieves dual occupancy of NET and SERT^[1].

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

Animal Model:

Sprague-Dawley (adult male, 150-220 g, formalin-induced inflammatory pain model)^[1]
Dosage:

10 mg/kg (esreboxetine); 1 mg/kg (Fluoxetine)
Administration:

i.p.; single dose
Result:

Produced 24% inhibition of flinching behavior in the rat formalin model.
Achieved 78% NET and 55% SERT ex vivo transporter occupancy at 75 minutes post-dose.
Shifted the morphine dose-response curve leftward, reducing the morphine ED₅₀ to 0.3 mg/kg, consistent with potentiation of morphine's antinociceptive effect.

Chemical Information

CAS No. 635724-55-9
Molecular Weight 431.48
Formula C₂₃H₂₉NO₇
SMILES

OC(CCC(O)=O)=O.CCOC(C=CC=C1)=C1O[C@H]([C@]2([H])CNCCO2)C3=CC=CC=C3
Synonyms

PNU-165442G; (S,S)-Reboxetine succinate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Shen F, et al. Relative contributions of norepinephrine and serotonin transporters to antinociceptive synergy between monoamine reuptake inhibitors and morphine in the rat formalin model. PloS one. 2013;8(9):e74891.

[2]. Fujimori I, et al. Design, synthesis and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitor. Bioorg Med Chem. 2015 Aug 1;23(15):5000-5014. [Content Brief]

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote