MK1064

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

MK1064 Chemical Structure

MK1064 Chemical Structure

CAS No. 1207253-08-4

Purity & Quality Control

MK1064 Related Products

Biological Activity

Description MK1064 is a selective orexin 2 receptor antagonist (2-SORA) with an IC50 of 18 nM.
Targets
orexin 2 receptor [1]
18 nM
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

Chemical Information & Solubility

Molecular Weight 461.90 Formula

C24H20ClN5O3

CAS No. 1207253-08-4 SDF --
Smiles COC1=C(OC)N=C(CNC(=O)C2=CC(=CN=C2C3=NC=CC=C3)C4=CC(=CN=C4)Cl)C=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 92 mg/mL ( (199.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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

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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
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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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