MK1064 - 98%, high purity , CAS No.1207253-08-4, Antagonist of OX 1 receptor;Antagonist of OX 2 receptor

Item Number
M413601
Grouped product items
SKUSizeAvailabilityPrice Qty
M413601-1mg
1mg
In stock
$78.90
M413601-5mg
5mg
In stock
$187.90
M413601-10mg
10mg
In stock
$305.90
M413601-25mg
25mg
In stock
$612.90
M413601-50mg
50mg
In stock
$899.90

OX Receptor Antagonists

Basic Description

SynonymsAC-36061 | BCP19608 | SB16800 | Urokinase inhibitor 1 | A16360 | AS-74199 | D84025 | GTPL9306 | 1207253-08-4 | CS-5968 | MK1064 | mk-1064 | UNII-O812716S9E | PENTAMIDINE ISETHIONATE [USP-RS] | BDBM50028059 | (2,2':5',3''-Terpyridine)-3'-carboxamide, 5''-c
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsMK1064 is a selective orexin\u20052 receptor antagonist (2-SORA) with an IC50 of 18 nM.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of OX 1 receptor;Antagonist of OX 2 receptor
Product Description

Information

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


Targets

orexin\u20052 receptor 18 nM

Product Properties

ALogP3.298
HBD Count1
Rotatable Bond7

Associated Targets(Human)

HCRTR1 Tclin Orexin receptor type 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HCRTR2 Tclin Orexin receptor type 2 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCRTR1 Tclin Orexin receptor 1 (5435 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
S1PR1 Tclin Sphingosine 1-phosphate receptor Edg-1 (5806 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GLP1R Tclin Glucagon-like peptide 1 receptor (111429 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
C5AR1 Tclin C5a anaphylatoxin chemotactic receptor (2677 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCRTR2 Tclin Orexin receptor 2 (5902 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Homo sapiens (32628 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CX3CR1 Tchem C-X3-C chemokine receptor 1 (1686 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FPR2 Tchem Lipoxin A4 receptor (3472 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FFAR4 Tchem G-protein coupled receptor 120 (2999 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GPR35 Tchem G-protein coupled receptor 35 (2643 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Aplnr Apelin receptor (201 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rhesus monkey (3147 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gpr119 Glucose-dependent insulinotropic receptor (270 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsome (341 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences
Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


FDA: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Other: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

ClinicalTrials: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DOI: [1]


Other: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1]


Names and Identifiers

IUPAC Name 5-(5-chloropyridin-3-yl)-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2-pyridin-2-ylpyridine-3-carboxamide
INCHI InChI=1S/C24H20ClN5O3/c1-32-21-7-6-18(30-24(21)33-2)14-29-23(31)19-10-16(15-9-17(25)13-26-11-15)12-28-22(19)20-5-3-4-8-27-20/h3-13H,14H2,1-2H3,(H,29,31)
InChi Key CKTWQGHVNRYNCM-UHFFFAOYSA-N
Canonical SMILES COC1=C(N=C(C=C1)CNC(=O)C2=C(N=CC(=C2)C3=CC(=CN=C3)Cl)C4=CC=CC=N4)OC
Isomeric SMILES COC1=C(N=C(C=C1)CNC(=O)C2=C(N=CC(=C2)C3=CC(=CN=C3)Cl)C4=CC=CC=N4)OC
PubChem CID 44633765
Molecular Weight 461.9

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot NumberCertificate TypeDateItem
H2213273Certificate of AnalysisJun 04, 2022 M413601
H2213283Certificate of AnalysisJun 04, 2022 M413601
H2213284Certificate of AnalysisJun 04, 2022 M413601
H2213285Certificate of AnalysisJun 04, 2022 M413601
H2213286Certificate of AnalysisJun 04, 2022 M413601

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 92 mg/mL (199.17 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility92
DMSO(mM) Max Solubility199.1773111063
Water(mg / mL) Max Solubility<1

Safety and Hazards(GHS)

Pictogram(s) GHS08
Signal Warning
Hazard Statements

H373:Causes damage to organs through prolonged or repeated exposure

H371:May cause damage to organs

Precautionary Statements

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P260:Do not breathe dust/fume/gas/mist/vapors/spray.

P270:Do not eat, drink or smoke when using this product.

P308+P316:IF exposed or concerned: Get emergency medical help immediately.

P319:Get medical help if you feel unwell.

Related Documents

References

1. Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, Lemaire W, Bruno JG, Harrell CM, Garson SL et al..  (2014)  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,  (2): (311-22).  [PMID:24376006] [10.1021/op500134e]
2. Gotter AL, Forman MS, Harrell CM, Stevens J, Svetnik V, Yee KL, Li X, Roecker AJ, Fox SV, Tannenbaum PL et al..  (2016)  Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man..  Sci Rep,  (13): (27147).  [PMID:27256922] [10.1021/op500134e]

Solution Calculators