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Merck
CN

V4629

(±)-维拉帕米 盐酸盐

≥99% (titration), powder, α1-adrenoceptor antagonist

别名:

5-[N-(3,4-二甲氧基苯基乙基)甲胺基]-2-(3,4-二甲氧基苯基)-2-异丙基戊腈α; 盐酸盐

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关于此项目

线性分子式:
(CH3O)2C6H3CH2CH2N(CH3)(CH2)3C[C6H3(OCH3)2][CH(CH3)2]CN · HCl
化学文摘社编号:
分子量:
491.06
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
205-800-5
MDL number:
Beilstein/REAXYS Number:
3647093
Assay:
≥99% (titration)
Form:
powder
Quality level:
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产品名称

(±)-维拉帕米 盐酸盐, ≥99% (titration), powder

Quality Level

assay

≥99% (titration)

form

powder

color

white

mp

142 °C (dec.) (lit.)

solubility

methanol: 50 mg/mL, ethanol: soluble

SMILES string

Cl.COc1ccc(CCN(C)CCCC(C#N)(C(C)C)c2ccc(OC)c(OC)c2)cc1OC

InChI

1S/C27H38N2O4.ClH/c1-20(2)27(19-28,22-10-12-24(31-5)26(18-22)33-7)14-8-15-29(3)16-13-21-9-11-23(30-4)25(17-21)32-6;/h9-12,17-18,20H,8,13-16H2,1-7H3;1H

InChI key

DOQPXTMNIUCOSY-UHFFFAOYSA-N

Application

盐酸维拉帕米已被用于:
  • 抑制受精卵中的钙振荡
  • 阻断钙通道,从而阻断 IL-1β(白细胞介素-1β)的作用,导致膜去极化
  • 研究维拉帕米对 1,3-二亚油酰甘油(DLG)细胞毒性的影响

Biochem/physiol Actions

α1-肾上腺素受体拮抗剂;L型钙通道阻滞剂。
α1-肾上腺素受体拮抗剂;L型钙通道阻滞剂。阻断平滑肌和心肌中的 L 型 Ca2+ 通道,体外诱导人原发性和转移性结肠癌细胞的凋亡。对 PGP 起作用的抗药性逆转剂,如减少肾小管清除地高辛。增加 Pgp 的基础 ATP 酶活性。Cyp3A4 和 CYP2C6 的底物。

Features and Benefits

该化合物在受体分类和信号转导手册的钙通道页面上有重点介绍。如需浏览其他手册页面,请点击此处
该化合物是ADME Tox研究的特色产品。点击此处 ,查看更多ADME Tox精选产品。了解更多有关用于其他研究领域的生物活性小分子的信息,请访问 sigma.com/discover-bsm


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pictograms

Skull and crossbonesEnvironment

signalword

Danger

hcodes

Hazard Classifications

Acute Tox. 3 Oral - Aquatic Chronic 2

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges



历史批次信息供参考:

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Françoise Nepveu et al.
Journal of medicinal chemistry, 53(2), 699-714 (2009-12-18)
A series of 66 new indolone-N-oxide derivatives was synthesized with three different methods. Compounds were evaluated for in vitro activity against CQ-sensitive (3D7), CQ-resistant (FcB1), and CQ and pyrimethamine cross-resistant (K1) strains of Plasmodium falciparum (P.f.), as well as for
Y Shiina et al.
Journal of reproduction and fertility, 97(1), 143-150 (1993-01-01)
Changes in intracellular calcium concentration ([Ca2+]i) in fertilized mouse oocytes were measured using the calcium-sensitive dye, fura-2. After fertilization, an initial long-lasting [Ca2+]i increase was followed by a periodic [Ca2+]i increase. The periodic increase in [Ca2+]i persisted for 1 to
O V Kolomytkin et al.
The American journal of physiology, 276(1 Pt 1), C9-C15 (1999-01-14)
The possibility that membrane depolarization of synovial fibroblasts caused by interleukin-1beta (IL-1beta) was mediated by protein kinase C (PKC) and Ca2+ influx was studied using inhibitor and activator analysis. The effect of IL-1beta was blocked by bisindolylmaleimide I, an inhibitor



全球贸易项目编号

货号GTIN
V4629-1G04061835516421
V4629-10G04061832964324
V4629-5G04061835559466