1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. Lemborexant

Lemborexant (Synonyms: E-2006)

Cat. No.: HY-16725 Purity: 99.92%
Handling Instructions

Lemborexant (E-2006) is a reversible, competitive and orally active dual antagonist of the orexin OX1 and OX2 receptors with IC50 values of 6.1 nM and 2.6 nM, respectively. Lemborexant can be treated insomnia.

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

Lemborexant Chemical Structure

Lemborexant Chemical Structure

CAS No. : 1369764-02-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 315 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 315 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 286 In-stock
Estimated Time of Arrival: December 31
10 mg USD 495 In-stock
Estimated Time of Arrival: December 31
25 mg USD 880 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lemborexant

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Lemborexant (E-2006) is a reversible, competitive and orally active dual antagonist of the orexin OX1 and OX2 receptors with IC50 values of 6.1 nM and 2.6 nM, respectively. Lemborexant can be treated insomnia[1].

IC50 & Target

OX1

6.1 nM (IC50)

OX2

2.6 nM (IC50)

In Vitro

A high-fat and high-calorie meal has been found to delay the time to peak levels by 2 hours. Its plasma protein binding in vitro is 94%. Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5[2].

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

In Vivo

Lemborexant is administered orally to pregnant rats during the period of organogenesis in 2 studies at doses of 60, 200, and 600 mg/kg/day or 20, 60, and 200 mg/kg/day, which are approximately 6 to >300 times the maximum recommended human dose (MRHD) based on AUC. Lemborexant causes maternal toxicity, manifests by decreased body weight and food consumption, decreases mean fetal body weight, an increased number of dead fetuses, and skeletal, external and visceral malformations (omphalocele, cleft palate, and membranous ventricular septal defect) at >300 times the MRHD based on AUC[2].
Lemborexant causes maternal toxicity that consisted of decreased body weight and food consumption and toxicity to offspring consisting of decreased pup body weights, decreases femur length, and decreases acoustic startle responses at 206 times the MRHD based on AUC. The no observed adverse effect levels (NOAEL) of 100 mg/kg/day is approximately 93 times the MRHD based on AUC[2].

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

Clinical Trial
Molecular Weight

410.42

Formula

C22H20F2N4O2

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (609.13 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4365 mL 12.1826 mL 24.3653 mL
5 mM 0.4873 mL 2.4365 mL 4.8731 mL
10 mM 0.2437 mL 1.2183 mL 2.4365 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution

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

Purity: 99.92%

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Lemborexant
Cat. No.:
HY-16725
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