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/ (+)-cis-Diltiazem HCl

硫氮酮 /(+)-cis-Diltiazem HCl {[allProObj[0].p_purity_real_show]}

货号：A198057 同义名： 盐酸地尔硫卓 / CRD-401;Diltiazem (hydrochloride)

Diltiazem HCl is a benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions.

(+)-cis-Diltiazem HCl 化学结构 CAS号：33286-22-5
(+)-cis-Diltiazem HCl 化学结构
CAS号：33286-22-5
(+)-cis-Diltiazem HCl 3D分子结构
CAS号：33286-22-5
(+)-cis-Diltiazem HCl 化学结构 CAS号：33286-22-5
(+)-cis-Diltiazem HCl 3D分子结构 CAS号：33286-22-5
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(+)-cis-Diltiazem HCl 纯度/质量文件 产品仅供科研

货号：A198057 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Ca2+ channel-like protein ↓ Calcium Channel ↓ Cav 2.2 ↓ 其他靶点 纯度
CDC25B-IN-2 ✔ Akt 99%+
Clevidipine ✔ 97%
Verapamil HCl ✔ 99%
Amlodipine ✔ 99%
Amlodipine maleate ✔ 98%
(+)-cis-Diltiazem HCl ✔ 95%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

 		99%+
Tanshinone IIA sulfonate sodium ✔ 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

 		99%+
Dronedarone Hydrochloride ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

 		98%
Efonidipine HCl monoethanolate ✔ 98%
Cinnarizine ✔ 98%
SEA0400 ++

NCX, IC50: 33 nM

 		ROS,ERK,p38 MAPK 99%+
Fasudil HCl ✔ Rho,PKA 98%
ML-9 ✔ Akt,MLCK 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

 		95%
Lomerizine 2HCl ✔ 98%
Efonidipine ✔ 98%
Levamlodipine ✔ 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

 		97%
Isradipine ✔ 98%
Lacidipine ✔ 98%
Lercanidipine ✔ 98%
Loureirin B ✔ Potassium Channel 99%+
Tetracaine HCl ✔ 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

 		98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

 		98%
Nicardipine ✔ 98%
Wilforgine ✔ 98+%
Econazole ✔ 99%+
Ginsenoside Rd ✔ NF-κB 98%
Fendiline HCl ✔ 98+%
Mesaconitine ✔ 98%
Tetrandrine ✔ 95%
Nifedipine ✔ 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

 		98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 98%
NP118809 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 μM

 		98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 98%
Cinepazide Maleate ✔ 98%
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Ranolazine ✔ 98%
Praeruptorin A ✔ Akt,p38 MAPK 98%
Ranolazine 2HCl ✔ 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

 		98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

 		98%
Levamlodipine besylate ✔ 97%
Carboxyamidotriazole Orotate ✔ 98%
IGS-1.76 ✔ 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

 		++++

Cav 2.2, IC50: 0.001 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

(+)-cis-Diltiazem HCl 生物活性

靶点

  • Calcium Channel
描述 Diltiazem hydrochloride, a benzothiazepine derivative, is antagonist of the calcium ion. Diltiazem caused a dose-dependent inhibiton of contractions as well as Ca++ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. There was a close relationship between diltiazem inhibition of Ca++ influx and inhibition of contraction when either 40 mM K+ or 10(-8) M NE (norepinephrine) was applied, but not when 10(-6) M NE was used. Also, diltiazem produced a noncompetitive inhibition of Ca++-induced contractions of depolarized rabbit aorta[3]. In conscious and anesthetized normotensive rats, intravenous administration of diltiazem (0.1 - 3 mg/kg) produced a dose-related decrease in blood pressure. Similarly, in conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreased the blood pressure and increased the heart rate after intravenous administration (0.03 - 1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduced the blood pressure of SHR. In addition, the progressive increase in blood pressure in young SHR was significantly suppressed by chronic oral administration of diltiazem (30 mg/kg)[4]. Diltiazem hydrochloride has beneficial effects on I/R (ischemia-reperfusion injury) injury, but this effect is weaker than cilostazol[5]. Diltiazem hydrochloride-loaded microsponges dispersed in rectal gels may be useful to overcome some limitations of conventional local chronic anal fissure therapy[6].

(+)-cis-Diltiazem HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02203630 Septic Shock ... 展开 >>Sepsis Shock Tachycardia Arrhythmia 收起 << Phase 4 Terminated(Slow enrollment; La... 展开 >>ck of support and equipoise) 收起 << - United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37232 收起 <<
NCT02203630 - Terminated(Slow enrollment; La... 展开 >>ck of support and equipoise) 收起 << - -
NCT00000620 Atherosclerosis ... 展开 >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease 收起 << Phase 3 Completed - United States, Minnesota ... 展开 >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada 收起 <<

(+)-cis-Diltiazem HCl 参考文献

[1]Freitas F, Estato V, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem, and propranolol. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40.

[2]Kraus RL, Hering S, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12.

[3]van Breemen C, Hwang O, Meisheri KD. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981; 218(2):459‐463

[4]Sato M, Murata S, Narita H, Tomita M, Yamashita K, Yamaguchi I. Nihon Yakurigaku Zasshi. 1979;75(2):99‐106

[5]Inan B, Sönmez Ergün S, Nurten A, et al. Effects of Cilostazol and Diltiazem Hydrochloride on Ischemia-Reperfusion Injury in a Rat Hindlimb Model. Heart Surg Forum. 2017;20(2):E058‐E065. Published 2017 Apr 29

[6]Ivanova NA, Trapani A, Franco CD, et al. In vitro and ex vivo studies on diltiazem hydrochloride-loaded microsponges in rectal gels for chronic anal fissures treatment. Int J Pharm. 2019; 557:53‐65

(+)-cis-Diltiazem HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.09mL

2.22mL

1.11mL

22.17mL

4.43mL

2.22mL

(+)-cis-Diltiazem HCl 技术信息

CAS号33286-22-5
分子式C22H27ClN2O4S
分子量 450.979
别名 盐酸地尔硫卓 ;CRD-401;Diltiazem (hydrochloride);(+)-cis-Diltiazem;RG 83606 HCl;Diltiazem HCl;Diltiazem hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

H2O: 30 mg/mL(66.52 mM)，配合低频超声助溶
动物实验配方

Tags: Diltiazem | 33286-22-5 | CRD-401 | CRD401 | CRD 401 | Calcium Channel Antagonist | Membrane Transporter/Ion Channel | Neuronal Signaling | Calcium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | (+)-cis-Diltiazem HCl 纯度/质量文件 | (+)-cis-Diltiazem HCl 亚型比较 | (+)-cis-Diltiazem HCl 生物活性 | (+)-cis-Diltiazem HCl 临床数据 | (+)-cis-Diltiazem HCl 参考文献 | (+)-cis-Diltiazem HCl 实验方案 | (+)-cis-Diltiazem HCl 技术信息

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