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

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(Human)

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)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SCN1A Tclin Sodium channel protein type I alpha subunit (483 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SCN5A Tclin Sodium channel protein type V alpha subunit (3462 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Scn2a Sodium channel protein type II alpha subunit (191 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn3a Sodium channel protein type III alpha subunit (24 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn9a Sodium channel protein type IX alpha subunit (69 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn8a Sodium channel protein type VIII alpha subunit (53 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn10a Sodium channel protein type X alpha subunit (425 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Scn4a Sodium channel protein type IV alpha subunit (55 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 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:

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

4 results found

Lot NumberCertificate TypeDateItem
K2117933Certificate of AnalysisSep 12, 2024 E174249
K2117934Certificate of AnalysisSep 12, 2024 E174249
K2117935Certificate of AnalysisSep 12, 2024 E174249
K2117937Certificate of AnalysisSep 12, 2024 E174249

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] [10.1021/op500134e]
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] [10.1021/op500134e]
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] [10.1021/op500134e]
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] [10.1021/op500134e]

Solution Calculators