Eleclazine hydrochloride

盐酸依拉嗪

BS-15137 | 1622226-81-6 | 4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazepin-5-one;hydrochloride | 4R1JP3Q4HI | GS 6615 hydrochlorideGS 6615 hydrochloride | 1448754-43-5 | UNII-4R1JP3Q4HI | Eleclazine hydrochloride | 1,4-

Eleclazine hydrochloride

E651613-5mg

5mg

≥99%

2-8°C储存,干燥

冰袋运输

Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC 50 value of In Vitro Eleclazine inhibits sodium current in hiPSC-derived cardiomyocytes with an IC 50 of 2.5 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Eleclazine (0.3 and 0.9 mg/kg; IV; infused over 15 minutes) reduces the incidence of epinephrine-induced ventricular premature beats and couplets, and shortens ventricular QT and atrial PTa intervals . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Yorkshire pigs (35.20 ± 0.46 kg; injected with epinephrine via a jugular vein) Dosage: 0.3 and 0.9 mg/kg Administration: IV; infused over 15 minutes Result: Reduced the incidence of epinephrine-induced ventricular premature beats and couplets by 51% (from 31.3 ± 1.91 to 15.2 ± 5.08 episodes; P = 0.038) and the incidence of 3- to 7-beat ventricular tachycardia (VT) by 56% (from 10.8 ± 3.45 to 4.7 ± 3.12 episodes; P = 0.004). Shortened ventricular QT and atrial PTa intervals by 7%, and reduced atrial repolarization alternans and heterogeneity without attenuation of the inotropic response to catecholamine. Form:Solid IC50& Target:Sodium current, Potassium current

盐酸榄香烯嗪（GS 6615）是一种选择性心脏晚期钠离子电流抑制剂，也是一种弱的钾离子电流抑制剂，其 IC 50 值分别小于 1 μM 和约 14.2 μM。盐酸榄香烯嗪再次显示出并发保护作用

1448754-43-5

C21H17ClF3N3O3

451.8 g/mol

90479986

C1COC2=C(C=C(C=C2)C3=CC=C(C=C3)OC(F)(F)F)C(=O)N1CC4=NC=CC=N4.Cl

4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazepin-5-one;hydrochloride

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

ZRYHNOXHGYUHFF-UHFFFAOYSA-N

C1COC2=C(C=C(C=C2)C3=CC=C(C=C3)OC(F)(F)F)C(=O)N1CC4=NC=CC=N4.Cl

90479986

DMSO : 50 mg/mL (110.66 mM; Need ultrasonic) H2O : <0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

1

8

4

451.091 Da

451.091 Da

64.599 Ų

31

0

578

0

2