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MK1064 OX Receptor antagonist

Name: MK1064
Brand: Selleck Chemicals
SKU: S6726
Rating: 5 (1 reviews)

Cat.No.S6726

MK1064 is a selective orexin 2 receptor antagonist (2-SORA) with an IC50 of 18 nM.

Chemical Structure

Molecular Weight: 461.90

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Quality Control

Batch: Purity: 99.70%

99.70

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other OX Receptor Inhibitors	Oveporexton (TAK-861) Almorexant HCl SB-334867 EMPA SB408124 TCS-OX2-29 Seltorexant

Chemical Information, Storage & Stability

Molecular Weight	461.90	Formula	C₂₄H₂₀ClN₅O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1207253-08-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=C(OC)N=C(CNC(=O)C2=CC(=CN=C2C3=NC=CC=C3)C4=CC(=CN=C4)Cl)C=C1

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	orexin 2 receptor 18 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/24376006/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02549027	Completed	Polysomnography	Merck Sharp & Dohme LLC	November 6 2009	Phase 1
NCT02549014	Completed	Pharmacokinetics	Merck Sharp & Dohme LLC	July 6 2009	Phase 1

Tech Support

Handling Instructions

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