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Product details

名称

Eleclazine hydrochloride

别名

盐酸依拉嗪

英文别名

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-

英文名称

Eleclazine hydrochloride

货号

E651613-5mg

包装规格

5mg

浓度

≥99%

储存温度

2-8°C储存,干燥

运输条件

冰袋运输

产品介绍

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

生化机理

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

CAS号

1448754-43-5

分子式

C21H17ClF3N3O3

分子量

451.8 g/mol

PubChem编号

90479986

Isomeric SMILES

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

IIUPAC Name

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

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

Smiles

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

PubChem CID

90479986

溶解性

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

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

451.091 Da

单同位素质量Monoisotopic Mass

451.091 Da

拓扑极表面积Topological Polar Surface Area

64.599 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

578

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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