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Merck
CN

D2521

(+)-顺式-地尔硫卓 盐酸盐

≥99% (HPLC), L-type Ca2+ channel blocker, powder

别名:

(2S,3S)-(+)-顺式-3-乙酰氧基-5-(2-二甲基氨基乙基)-2,3-二氢-2-(4-甲氧基苯基)-1,5-苯并硫氮杂-4(5H)- 酮 盐酸盐, CRD-401

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关于此项目

经验公式(希尔记法):
C22H26N2O4S · HCl
化学文摘社编号:
分子量:
450.98
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
251-443-3
MDL number:
Beilstein/REAXYS Number:
4228706
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
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产品名称

(+)-顺式-地尔硫卓 盐酸盐, ≥99% (HPLC)

InChI key

HDRXZJPWHTXQRI-BHDTVMLSSA-N

InChI

1S/C22H26N2O4S.ClH/c1-15(25)28-20-21(16-9-11-17(27-4)12-10-16)29-19-8-6-5-7-18(19)24(22(20)26)14-13-23(2)3;/h5-12,20-21H,13-14H2,1-4H3;1H/t20-,21+;/m1./s1

SMILES string

Cl.COc1ccc(cc1)[C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O

assay

≥99% (HPLC)

form

powder

originator

Valeant

storage temp.

2-8°C

Quality Level

Gene Information

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Application

(+)-顺式-盐酸地尔硫卓已用于:
  • 研究其对整体分散基质(monolithic dispersion matrix)中扩散和释放的影响(26)
  • 研究其在视网膜色素变性(RP)模型中的神经保护作用(27)
  • 作为Cav1.2 L型钙通道(LTCC)的拮抗剂(28)

Biochem/physiol Actions

封闭缓慢或L-型Ca2+通道;调节来自中性粒细胞内存储的Ca2+的释放;刺激1,4-二氢吡啶结合至Ca2+通道;冠状动脉舒张剂。

Features and Benefits

该化合物在受体分类和信号转导手册的 钙通道环核苷酸门控(CNG)和超极化激活的环核苷酸门控(HCN)通道 页面上有详细描述。如需浏览其他手册页面,请点击此处
该化合物由Valeant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
这种化合物是环核苷酸研究的特色产品。点击此处发现更多特色环核苷酸产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

General description

盐酸地尔硫卓可用于治疗心血管疾病,例如心绞痛和高血压。它可充当细胞色素P450 3A(CYP3A)的抑制剂。地尔硫卓可能与斑丘疹、荨麻疹和瘙痒有关。

pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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M J Gunthorpe et al.
The Journal of physiology, 519 Pt 3, 713-722 (1999-08-24)
1. To extend our knowledge of the site and mechanism of action of L-type Ca2+ channel antagonists on 5-HT3 receptors, whole-cell voltage clamp electrophysiology was used to investigate the action of one of these compounds, diltiazem, on the recombinant receptor
Andrés Pizzorno et al.
Cell reports. Medicine, 1(4), 100059-100059 (2020-08-25)
In the current COVID-19 pandemic context, proposing and validating effective treatments represents a major challenge. However, the scarcity of biologically relevant pre-clinical models of SARS-CoV-2 infection imposes a significant barrier for scientific and medical progress, including the rapid transition of
Determination of plasma protein binding of diltiazem in horses by ultrafiltration.
C C Schwarzwald et al.
Journal of veterinary pharmacology and therapeutics, 29(6), 579-580 (2006-11-07)
Effect of diltiazem on midazolam and alfentanil disposition in patients undergoing coronary artery bypass grafting
Ahonen J, et al.
Anesthesiology, 85(6), 1246-1252 (1996)
D Dobrev et al.
British journal of pharmacology, 127(2), 576-582 (1999-06-29)
1. The putative inhibitory effects of verapamil and diltiazem on neuronal non-L-type Ca2+ channels were studied by investigating their effects on either K+- or veratridine-evoked [3H]-dopamine ([3H]-DA) release in rat striatal slices. Involvement of N-, P- and Q-type channels was

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