2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. MK-1064

MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia.

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

MK-1064 Chemical Structure

MK-1064 Chemical Structure

CAS No. : 1207253-08-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 138 In-stock
Solution
10 mM * 1 mL in DMSO USD 138 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 125 In-stock
10 mg USD 200 In-stock
25 mg USD 365 In-stock
50 mg USD 590 In-stock
100 mg USD 950 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

MK-1064 Related Antibodies

Top Publications Citing Use of Products

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OX2 Receptor OX1 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia[1][3].

IC50 & Target[1]

OX2 Receptor

18 nM (IC50)

OX1 Receptor

1789 nM (IC50)

OX2 Receptor

0.5 nM (Ki)

OX1 Receptor

1584 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
1789 nM
Compound: 66; MK-1064
Antagonist activity at human OX1R expressed in CHO cells by FLIPR assay
Antagonist activity at human OX1R expressed in CHO cells by FLIPR assay
[PMID: 26317591]
CHO IC50
18 nM
Compound: 66; MK-1064
Antagonist activity at human OX2R expressed in CHO cells by FLIPR assay
Antagonist activity at human OX2R expressed in CHO cells by FLIPR assay
[PMID: 26317591]
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].

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

Animal Model: Wild-type and OX2R 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) t1/2 (h) Dose (mg/kg) Cmax (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
Molecular Weight

461.90

Formula

C24H20ClN5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(C2=CC(Cl)=CN=C2)=CN=C1C3=NC=CC=C3)NCC4=NC(OC)=C(OC)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (108.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1650 mL 10.8249 mL 21.6497 mL 54.1243 mL
5 mM 0.4330 mL 2.1650 mL 4.3299 mL 10.8249 mL
10 mM 0.2165 mL 1.0825 mL 2.1650 mL 5.4124 mL
15 mM 0.1443 mL 0.7217 mL 1.4433 mL 3.6083 mL
20 mM 0.1082 mL 0.5412 mL 1.0825 mL 2.7062 mL
25 mM 0.0866 mL 0.4330 mL 0.8660 mL 2.1650 mL
30 mM 0.0722 mL 0.3608 mL 0.7217 mL 1.8041 mL
40 mM 0.0541 mL 0.2706 mL 0.5412 mL 1.3531 mL
50 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0825 mL
60 mM 0.0361 mL 0.1804 mL 0.3608 mL 0.9021 mL
80 mM 0.0271 mL 0.1353 mL 0.2706 mL 0.6766 mL
100 mM 0.0216 mL 0.1082 mL 0.2165 mL 0.5412 mL
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MK-1064 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-10641207253-08-4MK1064MK 1064Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorSleepinsomniaOX2R knockoutstressInhibitorinhibitorinhibit

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