MK-1064
Based on 3 publication(s) in Google Scholar
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.
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- Purity : 99.95%
- CAS No.: 1207253-08-4
- 화학식: C24H20ClN5O3
- 분자량:461.90
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MK-1064
MoreAll Orexin Receptor (OX Receptor) Isoforms
More
Biological Activity
제품 설명
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
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
1789 nM
Compound: 66; MK-1064
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Antagonist activity at human OX1R expressed in CHO cells by FLIPR assay
Antagonist activity at human OX1R expressed in CHO cells by FLIPR assay
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[PMID: 26317591] |
| CHO | IC50 |
18 nM
Compound: 66; MK-1064
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Antagonist activity at human OX2R expressed in CHO cells by FLIPR assay
Antagonist activity at human OX2R expressed in CHO cells by FLIPR assay
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[PMID: 26317591] |
In Vivo
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.
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Animal Model:Wild-type and OX2R knockout mice[2]
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Dosage:30 mg/kg
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Administration:Oral administration
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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.
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Animal Model:Rat, dog, and rhesus monkey (Pharmacokinetics assay)[1]
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Dosage:1, 2, 3, 5 mg/kg
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Administration:Oral administration (P.O.), intravenous injection (I.V.)
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1207253-08-4
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Appearance Solid
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분자량 461.90
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화학식 C24H20ClN5O3
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC(Cl)=CN=C2)=CN=C1C3=NC=CC=C3)NCC4=NC(OC)=C(OC)C=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Neuropharmacology
Contextual generalization of social stress learning is modulated by orexin receptors in basolateral amygdala. [Abstract]2022 Sep 1:215:109168. PMID: 35724928 -
Neuropharmacology
Orexin 2 receptor stimulation enhances resilience, while orexin 2 inhibition promotes susceptibility, to social stress, anxiety and depression. [Abstract]2018 Dec:143:79-94. PMID: 30240784 -
bioRxiv
Prioritizing Neuroactive Ligands Using Motif-Guided Virtual Discovery and Zebrafish Profiling. [Abstract]2026 Jan 16:2026.01.15.699747. PMID: 41648545
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Roecker AJ et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. ChemMedChem. 2014 Feb;9(2):311-22. [Content Brief]
[2]. Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147. [Content Brief]
[3]. Laura A Grafe, et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience. 2017 Apr 21;348:313-323. [Content Brief]
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 |
MK-1064 Related Classifications
HY-19914 Related Classifications
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