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

MK-1064 

Cat. No.: HY-19914 Purity: 99.48%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 219 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 219 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 310 In-stock
Estimated Time of Arrival: December 31
25 mg USD 620 In-stock
Estimated Time of Arrival: December 31
50 mg USD 910 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 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)

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 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.
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 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.
Purity & Documentation
References
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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.

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Product Name:
MK-1064
Cat. No.:
HY-19914
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