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

Filorexant (Synonyms: MK-6096)

Cat. No.: HY-15653 Purity: 98.95%
Handling Instructions

Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).

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

Filorexant Chemical Structure

Filorexant Chemical Structure

CAS No. : 1088991-73-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 198 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1176 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).

IC50 & Target

Ki: < 3 nM(Orexin receptor)[1].

In Vitro

In radioligand binding and functional cell based assays Filorexant (MK-6096) demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes. Filorexant (MK-6096) occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM.

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

In Vivo

Filorexant (MK-6096) dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg).

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

Clinical Trial
Molecular Weight

420.48

Formula

C₂₄H₂₅FN₄O₂

CAS No.
SMILES

CC1=CC(C(N2C[[email protected]](COC3=CC=C(F)C=N3)CC[[email protected]]2C)=O)=C(C4=NC=CC=N4)C=C1

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 : 12.61 mg/mL (29.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3782 mL 11.8912 mL 23.7823 mL
5 mM 0.4756 mL 2.3782 mL 4.7565 mL
10 mM 0.2378 mL 1.1891 mL 2.3782 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Animal administration[1]
The male Sprague Dawley rats (n = 8/study; age: 3-6 months; weight: 450-600 g) were singly housed with water and food ad libitum and a 12 h light: 12 h dark cycle with lights on at 04:00 and off at 16:00. Sleep studies were conducted to evaluate Filorexant (3 and 10 mg/kg, p.o.), DORA-22 (10 mg/kg, p.o.) and almorexant (3 and 30 mg/kg, p.o.), employing a counterbalanced crossover design in which all animals were alternatively treated with drug and vehicle daily for either 3 or 7 consecutive days (for DORA-22 and Filorexant, respectively): 2 baseline days (no dosing), a 2 day vehicle-only run-in, a 3 or 7-day arm of drug or vehicle followed by 3 or 7 days of conditional crossover. Effects of compound treatments relative to vehicle (20% Vitamin E TPGS, p.o.) were evaluated following administration in the active phase).

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

References
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Keywords:

FilorexantMK-6096MK6096MK 6096Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorInhibitorinhibitorinhibit

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Filorexant
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