Click Here for 5% Off Your First Aladdin Purchase!

Eleclazine - 97%, high purity , CAS No.1443211-72-0, Inhibitor of Na v1.5

  • Moligand™
  • ≥97%
Item Number
E174249
Grouped product items
SKUSizeAvailabilityPrice Qty
E174249-5mg
5mg
In stock
$36.90
E174249-25mg
25mg
In stock
$153.90
E174249-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$510.90
E174249-250mg
250mg
In stock
$946.90
View related series
Nav1.5 Inhibitor

Basic Description

SynonymsEleclazine|1443211-72-0|GS-6615|Eleclazine [INN]|4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one|PUY08529FK|4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazepin-5-one|1,4-B
Specifications & PurityMoligand™, ≥97%
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of Na v1.5
Product Description

Product Application:

ELECLAZINE is a late sodium current inhibitor and a phase II agent with demonstrated pre-clinical anti-ischemic and antiarrhythmic properties.

Associated Targets

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C8 Tchem Cytochrome P450 2C8 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2B6 Tchem Cytochrome P450 2B6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN2A Tclin Sodium channel protein type 2 subunit alpha 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN5A Tclin Sodium channel protein type 5 subunit alpha 6 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN10A Tclin Sodium channel protein type 10 subunit alpha 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN3A Tclin Sodium channel protein type 3 subunit alpha 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN9A Tclin Sodium channel protein type 9 subunit alpha 6 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN4A Tclin Sodium channel protein type 4 subunit alpha 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN1A Tclin Sodium channel protein type 1 subunit alpha 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN8A Tclin Sodium channel protein type 8 subunit alpha 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazepin-5-one
INCHI InChI=1S/C21H16F3N3O3/c22-21(23,24)30-16-5-2-14(3-6-16)15-4-7-18-17(12-15)20(28)27(10-11-29-18)13-19-25-8-1-9-26-19/h1-9,12H,10-11,13H2
InChi Key YNUAEEJQYHYLMS-UHFFFAOYSA-N
Canonical SMILES C1COC2=C(C=C(C=C2)C3=CC=C(C=C3)OC(F)(F)F)C(=O)N1CC4=NC=CC=N4
Isomeric SMILES C1COC2=C(C=C(C=C2)C3=CC=C(C=C3)OC(F)(F)F)C(=O)N1CC4=NC=CC=N4
PubChem CID 71183216
Molecular Weight 415.372

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Chemical and Physical Properties

SolubilityDMSO (Slightly), Methanol (Slightly)
Melt Point(°C)72 - 74°C

Related Documents

References

1. Grasberger BL, Lu T, Schubert C, Parks DJ, Carver TE, Koblish HK, Cummings MD, LaFrance LV, Milkiewicz KL, Calvo RR et al..  (2005)  Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells..  J Med Chem,  48  (4): (909-12).  [PMID:15715460]
2. Raboisson P, Marugán JJ, Schubert C, Koblish HK, Lu T, Zhao S, Player MR, Maroney AC, Reed RL, Huebert ND et al..  (2005)  Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists..  Bioorg Med Chem Lett,  15  (7): (1857-61).  [PMID:15780621]
3. Antuch W, Menon S, Chen QZ, Lu Y, Sakamuri S, Beck B, Schauer-Vukasinović V, Agarwal S, Hess S, Dömling A.  (2006)  Design and modular parallel synthesis of a MCR derived alpha-helix mimetic protein-protein interaction inhibitor scaffold..  Bioorg Med Chem Lett,  16  (6): (1740-3).  [PMID:16427279]
4. Cummings MD, Schubert C, Parks DJ, Calvo RR, LaFrance LV, Lattanze J, Milkiewicz KL, Lu T.  (2006)  Substituted 1,4-benzodiazepine-2,5-diones as alpha-helix mimetic antagonists of the HDM2-p53 protein-protein interaction..  Chem Biol Drug Des,  67  (3): (201-5).  [PMID:16611213]

Solution Calculators