[CAS NO. 1088991-73-4] Filorexant

Name: Filorexant
Brand: Arctom Scientific
SKU: AS943089

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PRODUCTS SPECIFICATIONS [1088991-73-4]

Fulfillment

Catalog

AS943089

Brand

Arctom Scientific

CAS

1088991-73-4

DESCRIPTION [1088991-73-4]

Overview

MDL	MFCD28100674
Molecular Weight	420.48
Molecular Formula	C24H25FN4O2
SMILES	CC1=CC(C(N2C[C@H](COC3=CC=C(F)C=N3)CC[C@H]2C)=O)=C(C4=NC=CC=N4)C=C1

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

Summary

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01564459	Merck Sharp & Dohme LLC	Diabetic Neuropathy, Painful	March 26, 2012	Phase 2
NCT01513291	Merck Sharp & Dohme LLC	Migraine\|Headache	February 6, 2012	Phase 2
NCT01021852	Merck Sharp & Dohme LLC	Primary Insomnia	November 30, 2009	Phase 2
NCT02549027	Merck Sharp & Dohme LLC	Polysomnography	November 6, 2009	Phase 1
NCT01554176	Merck Sharp & Dohme LLC	Major Depressive Disorder, Recurrent	May 18, 2012	Phase 2

Appearance

Solid

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 : 100 mg/mL ( 237.82 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 available by MCE.

References

Synonyms

Methanone, [(2R,5R)-5-[[(5-fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]-

[(2R,5R)-5-[[(5-Fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]methanone

MK 6096

Filorexant