[CAS NO. 1207253-08-4] MK-1064

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PRODUCTS SPECIFICATIONS [1207253-08-4]

Catalog

HY-19914

Brand

MCE

CAS

1207253-08-4

DESCRIPTION [1207253-08-4]

Overview

MDL	MFCD28502027
Molecular Weight	461.90
Molecular Formula	C24H20ClN5O3
SMILES	O=C(C1=CC(C2=CC(Cl)=CN=C2)=CN=C1C3=NC=CC=C3)NCC4=NC(OC)=C(OC)C=C4

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

2 Publications Citing Use of MCE

Summary

MK-1064 is a selective and orally active OX ₂ R antagonist ( K _i : 0.5 nM, IC ₅₀ : 18 nM). MK-1064 promotes sleep in vivo . MK-1064 can be used in the research of insomnia ^[1] ^[3] .

IC50 & Target

OX ₂ Receptor

18 nM (IC ₅₀ )

OX ₁ Receptor

1789 nM (IC ₅₀ )

OX ₂ Receptor

0.5 nM (Ki)

OX ₁ Receptor

1584 nM (Ki)

In Vivo

MK-1064 (30 mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice ^[2] .
MK-1064 (30 mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats ^[3] .
MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey ^[1] .

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

Animal Model:	Wild-type and OX ₂ R knockout mice ^[2]
Dosage:	30 mg/kg
Administration:	Oral administration
Result:	Displayed active wake reduction accompanied by significant increases in SWS (slow-wave sleep) and REM (rapid eye movement) at time points up to 3.5 hours following treatment.

Animal Model:

Rat, dog, and rhesus monkey (Pharmacokinetics assay) ^[1]

Dosage:

1, 2, 3, 5 mg/kg

Administration:

Oral administration (P.O.), intravenous injection (I.V.)

Result:

Pharmacokinetics profile of MK-1064.

Species	Dose (mg/kg)	CL (mL/min/kg)	t _1/2 (h)	Dose (mg/kg)	C _max (μM)	F (%)
Rat	2 (I.V.)	39	0.3	5 (P.O.)	1.5	54
Dog	1 (I.V.)	16	1.0	3 (P.O.)	1.0	48
Rhesus	2 (I.V.)	12	0.8	5 (P.O.)	0.9	16

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02549027	Merck Sharp & Dohme LLC	Polysomnography	November 6, 2009	Phase 1
NCT02549014	Merck Sharp & Dohme LLC	Pharmacokinetics	July 6, 2009	Phase 1

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 : 50 mg/mL ( 108.25 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1650 mL	10.8249 mL	21.6497 mL
5 mM	0.4330 mL	2.1650 mL	4.3299 mL
10 mM	0.2165 mL	1.0825 mL	2.1650 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 (5.41 mM); Clear solution

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