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R6152

Sigma-Aldrich

雷诺嗪 二盐酸盐

≥98% (HPLC), powder, Na⁺-current blocker

同義詞:

(±)-4- [2-羟基-3-(邻甲氧基苯氧基)丙基]-1-哌嗪乙酰-2′,6'-二甲苯胺 二盐酸盐, N-(2,6-二甲基苯基)-4-[2-羟基-3-(2-甲氧基苯氧基)丙基]-1-哌嗪乙酰胺 二盐酸盐

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About This Item

經驗公式(希爾表示法):
C24H33N3O4 · 2HCl
CAS號碼:
分子量::
500.46
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

product name

雷诺嗪 二盐酸盐, ≥98% (HPLC), powder

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

mp

222-229.5 °C (lit.)

溶解度

H2O: soluble ≥10 mg/mL

起源

Gilead

SMILES 字串

Cl.Cl.COc1ccccc1OCC(O)CN2CCN(CC2)CC(=O)Nc3c(C)cccc3C

InChI

1S/C24H33N3O4.2ClH/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3;;/h4-10,20,28H,11-17H2,1-3H3,(H,25,29);2*1H

InChI 密鑰

RJNSNFZXAZXOFX-UHFFFAOYSA-N

基因資訊

應用

盐酸雷诺嗪已被用作:
  • 低尖端扭转(TdP)风险药物,以研究其对犬心血管模型QTc延长、心电图(PR和QRS)间期的影响
  • 部分脂肪酸氧化(FAO)抑制剂,以研究其对胶质母细胞瘤细胞的作用
  • 晚期钠(Na+)-电流抑制剂,以研究其对兔心房性心动过速的影响。

生化/生理作用

雷诺嗪是抗局部缺血哌嗪的衍生物,可作为钠(Na+)-电流抑制剂。它具有治疗舒张性心力衰竭和改善心肌舒张功能的潜力。
pFOX(部分脂肪酸氧化)抑制剂是一类新型的抗心绞痛药物,可抑制脂肪酸β-氧化并激活丙酮酸脱氢酶,从而使心脏的能量从脂质转移到葡萄糖,氧气消耗更少,并有助于在缺血时维持心肌功能。

特點和優勢

该化合物由Gilead开发。要浏览其他药物开发化合物和批准的药物/候选药物列表,单击此处

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


分析證明 (COA)

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Irene Del-Canto et al.
Frontiers in physiology, 11, 922-922 (2020-08-28)
Mechanical stretch increases Na+ inflow into myocytes, related to mechanisms including stretch-activated channels or Na+/H+ exchanger activation, involving Ca2+ increase that leads to changes in electrophysiological properties favoring arrhythmia induction. Ranolazine is an antianginal drug with confirmed beneficial effects against
Leigh D Plant et al.
Cell reports, 30(7), 2225-2236 (2020-02-23)
Acute cardiac hypoxia produces life-threatening elevations in late sodium current (ILATE) in the human heart. Here, we show the underlying mechanism: hypoxia induces rapid SUMOylation of NaV1.5 channels so they reopen when normally inactive, late in the action potential. NaV1.5
Isaac Aidonidis et al.
The Journal of innovations in cardiac rhythm management, 12(3), 4421-4427 (2021-03-30)
Ranolazine (RAN) has previously been shown to lower the onset of cholinergic atrial fibrillation in intact animals; however, its efficacy in the setting of atrial tachycardia (AT) is unknown. The purpose of this study was to investigate the effects of
Aya Nagaoka et al.
The Journal of biological chemistry, 290(52), 30910-30923 (2015-11-01)
Regulation of hyaluronan (HA) synthesis and degradation is essential to maintenance of extracellular matrix homeostasis. We recently reported that HYBID (HYaluronan-Binding protein Involved in hyaluronan Depolymerization), also called KIAA1199, plays a key role in HA depolymerization in skin and arthritic
Kelly J McKelvey et al.
Frontiers in oncology, 11, 633210-633210 (2021-04-16)
Glioblastoma (GBM) is the most aggressive adult glioma with a median survival of 14 months. While standard treatments (safe maximal resection, radiation, and temozolomide chemotherapy) have increased the median survival in favorable O(6)-methylguanine-DNA methyltransferase (MGMT)-methylated GBM (~21 months), a large

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