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862309-06-6 (MK-0249)

1

Identification

MK-0249 MK-0249
Name MK-0249
Formula C23H24F3N3O2
MW 431.45
CAS No. 862309-06-6
EINECS
Smiles O=C1N(C2=CC=C(OCCCN3CCCC3)C=C2)C(C)=NC4=C1C(C(F)(F)F)=CC=C4
Synonyms MK0249;MK 0249; 2-methyl-3-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)-5-(trifluoromethyl)quinazolin-4(3H)-one
InChI InChI=1S/C23H24F3N3O2/c1-16-27-20-7-4-6-19(23(24,25)26)21(20)22(30)29(16)17-8-10-18(11-9-17)31-15-5-14-28-12-2-3-13-28/h4,6-11H,2-3,5,12-15H2,1H3
2

Introduction

MK-0249 is a potent histamine H3 receptor antagonist, with Ki of 1.7 nM for human H3.

Background Information

MK-0249 is a potent histamine H3 receptor antagonist, with Ki of 1.7 nM for human H3. ......by MedChemexpress Co., Ltd.
MK-0249 is a histamine H3 inverse antagonist. Current antipsychotic treatments have little impact on the cognitive deficits associated with schizophrenia. It has been proposed that agents which promote histamine release may enhance cognition and, therefore, the H3 inverse agonist MK-0249 might improve cognitive deficits in patients with schizophrenia. ......by MedKoo Biosciences, Inc.
MK-0249 is a histamine H3 receptor antagonist potentially for the treatment of schizophrenia, and Alzheimer's disease. ......by MedKoo Biosciences, Inc.
MK-0249 is a novel potent, selective histamine H3 inverse agonist for the treatment of cognitive impairment with schizophrenia.Sleep DisorderPhase 1 Discontinued ......by ProbeChem
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000126444

Storage condition

Solubility

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Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
MK-0249 Merck Sharp & Dohme Corp. Alzheimer's Disease|Dementia 2009/4/1 Phase 1
MK-0249 Merck Sharp & Dohme Corp. Paranoid Schizophrenia 2007/12/1 Phase 2
MK-0249 Merck Sharp & Dohme Corp. Alzheimer's Disease 2006/11/1 Phase 2
MK-0249 Merck Sharp & Dohme Corp. Sleep Apnea, Obstructive|Hypopnea Syndrome|Excessive Daytime Sleepiness 2008/2/1 Phase 2
MK-0249 Merck Sharp & Dohme Corp. Attention-Deficit/Hyperactivity Disorder (ADHD) 2007/7/1 Phase 2
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Safety Data of MK-0249

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC 1mg/USD696();5mg/USD1380() USA
MedChemexpress Co., Ltd. 1mg/USD696();5mg/USD1380() USA
MedKoo Biosciences, Inc. USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 1mg/USD696();5mg/USD1380() China
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Related Products

Other Forms of 862309-06-6

Name CAS No Formula MW

Recommended Compounds in Histamine Receptor

Name CAS No Formula MW
Doxylamine (succinate) 562-10-7 C21H28N2O5 388.46
Ebastine 90729-43-4 C32H39NO2 469.66
Azelastine 58581-89-8 C22H24ClN3O 381.9
Epinastine 80012-43-7 C16H15N3 249.31
Hydroxyzine (dihydrochloride) 2192-20-3 C21H29Cl3N2O2 447.83
Hydroxyzine 68-88-2 C21H27ClN2O2 374.9
Desloratadine 100643-71-8 C19H19ClN2 310.82
Pemirolast (potassium) 100299-08-9 C10H7KN6O 266.3
Betahistine (dihydrochloride) 5579-84-0 C8H14Cl2N2 209.12
Brompheniramine (maleate) 980-71-2 C20H23BrN2O4 435.31
Azelastine (hydrochloride) 79307-93-0 C22H25Cl2N3O 418.36
Olopatadine (hydrochloride) 140462-76-6 C21H24ClNO3 373.87
Famotidine 76824-35-6 C8H15N7O2S3 337.45
Meclizine (dihydrochloride) 1104-22-9 C25H29Cl3N2 463.87
Nizatidine 76963-41-2 C12H21N5O2S2 331.46
Roxatidine (Acetate Hydrochloride) 93793-83-0 C19H29ClN2O4 384.9
Diphenhydramine (hydrochloride) 147-24-0 C17H22ClNO 291.82
Clemastine (fumarate) 14976-57-9 C25H30ClNO5 459.96
Chlorpheniramine (maleate) 113-92-8 C20H23ClN2O4 390.86
Ranitidine (hydrochloride) 66357-59-3 C13H23ClN4O3S 350.86

Recommended Compounds in Same Indication

Name CAS No Formula MW
CHF5074 749269-83-8 C16H11Cl2FO2 325.1617
Azeliragon 603148-36-3 C32H38ClN3O2 532.116
LY451395 375345-95-2 C21H30N2O4S2 438.6
MSDC 0160 146062-49-9 C19H18N2O4S 370.42
THK5351 1707147-26-9 C18H18FN3O2 0.0
Scopolamine 51-34-3 C17H21NO4 303.35
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Route of Synthesis

12

References

Protocol Reference

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More Information

MK-0249

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