TCS OX2 29 - 95%, high purity , CAS No.372523-75-6, Antagonist of OX 2 receptor

Item Number
T275857
Grouped product items
SKUSizeAvailabilityPrice Qty
T275857-5mg
5mg
In stock
$78.90
T275857-10mg
10mg
In stock
$117.90
T275857-25mg
25mg
In stock
$226.90
T275857-50mg
50mg
In stock
$335.90
T275857-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$593.90
T275857-250mg
250mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$1,336.90

Potent, selective orexin-2 receptor antagonist

Basic Description

Synonyms(2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-((4-pyridinylmethyl)amino)-1-butanone | AKOS032944970 | NCGC00370876-01 | KB-11822 | DTXSID801028419 | Isoquinoline, 2-((2S)-3,3-dimethyl-1-oxo-2-((4-pyridinylmethyl)amino)butyl)-1,2,3,
Specifications & PurityMoligand™, ≥95%
Biochemical and Physiological MechanismsTCS OX2 29 or TCS-OX2-29 is a potent and selective orexin 2 receptor (Ox2R, Ox2-R, Ox-2-R) antagonist (IC50 = 40 nM/Ox2R, >10 μM/Ox1R) with little potency toward 50 other receptors, ion channels, and transporters tested (<30% inhibition at 10 μM). TCS OX2
SourceSynthetic
Storage TempStore at -20°C,Desiccated
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of OX 2 receptor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.

Associated Targets(Human)

HCRTR2 Tclin Orexin receptor type 2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HCRTR1 Tclin Orexin receptor 1 (5435 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCRTR2 Tclin Orexin receptor 2 (5902 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (2S)-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethyl-2-(pyridin-4-ylmethylamino)butan-1-one
INCHI InChI=1S/C23H31N3O3/c1-23(2,3)21(25-14-16-6-9-24-10-7-16)22(27)26-11-8-17-12-19(28-4)20(29-5)13-18(17)15-26/h6-7,9-10,12-13,21,25H,8,11,14-15H2,1-5H3/t21-/m1/s1
InChi Key COFVZFLCAOUMJT-OAQYLSRUSA-N
Canonical SMILES CC(C)(C)C(C(=O)N1CCC2=CC(=C(C=C2C1)OC)OC)NCC3=CC=NC=C3
Isomeric SMILES CC(C)(C)[C@@H](C(=O)N1CCC2=CC(=C(C=C2C1)OC)OC)NCC3=CC=NC=C3
PubChem CID 10408514
Molecular Weight 397.5

Certificates

Certificate of Analysis(COA)

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6 results found

Lot NumberCertificate TypeDateItem
B2225044Certificate of AnalysisSep 20, 2023 T275857
B2225045Certificate of AnalysisSep 20, 2023 T275857
B2225047Certificate of AnalysisSep 20, 2023 T275857
B2225051Certificate of AnalysisSep 20, 2023 T275857
B2225146Certificate of AnalysisSep 20, 2023 T275857
B2225151Certificate of AnalysisSep 20, 2023 T275857

Chemical and Physical Properties

SolubilitySoluble in water to 100 mM and in DMSO to 10mM

Related Documents

References

1. Hirose M, Egashira S, Goto Y, Hashihayata T, Ohtake N, Iwaasa H, Hata M, Fukami T, Kanatani A, Yamada K.  (2003)  N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist..  Bioorg Med Chem Lett,  13  (24): (4497-9).  [PMID:14643355] [10.1021/op500134e]

Solution Calculators