Eleclazine HCl

CAS
1448754-43-5
Catalog Number
ACM1448754435
Category
Inhibitors
Molecular Weight
451.83
Molecular Formula
C21H17ClF3N3O3

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Specification

Description
Eleclazine HCl is a novel late Na+ current inhibitor.
Synonyms
Eleclazine Hydrochloride; Eleclazine HCl; GS-6615; GS 6615; GS6615
IUPAC Name
4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one hydrochloride
Canonical SMILES
O=C1N(CC2=NC=CC=N2)CCOC3=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=C13.[H]Cl
InChI
InChI=1S/C21H16F3N3O3.ClH/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;1H
InChI Key
ZRYHNOXHGYUHFF-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Appearance
Solid powder
Shelf Life
>3 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Alternative CAS
1443211-72-0 (free base); 1448754-43-5 (HCl)
Biological Target
Eleclazine hydrochloride is a novel late Na+ current inhibitor with IC50 value of 0.7 uM.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 55.82; H, 3.79; Cl, 7.85; F, 12.61; N, 9.30; O, 10.62
Exact Mass
451.0911
HS Tariff Code
2934.99.03.00
In Vitro Activity
TBD
In Vivo Activity
Eleclazine (10 μM) inhibited INa in atrial and ventricular myocytes in a use-dependent manner consistent with preferential activated state block. Eleclazine produced voltage-dependent instantaneous inhibition in atrial and ventricular myocytes; it caused a negative shift in voltage of half-maximal inactivation and slowed the recovery of INa from inactivation in both cell types.
Reference: Heart Rhythm O2. 2020 Aug;1(3):206-214. https://pubmed.ncbi.nlm.nih.gov/32864638/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
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