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/ (+)-cis-Diltiazem HCl/硫氮酮

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

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

(+)-cis-Diltiazem HCl是苯并噻唑啉类衍生物，具有血管扩张作用，因其拮抗钙离子在细胞膜中的作用。

(+)-cis-Diltiazem HCl/硫氮酮 化学结构 CAS号：33286-22-5
(+)-cis-Diltiazem HCl/硫氮酮 化学结构
CAS号：33286-22-5
(+)-cis-Diltiazem HCl/硫氮酮 3D分子结构
CAS号：33286-22-5
(+)-cis-Diltiazem HCl/硫氮酮 化学结构 CAS号：33286-22-5
(+)-cis-Diltiazem HCl/硫氮酮 3D分子结构 CAS号：33286-22-5
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(+)-cis-Diltiazem HCl/硫氮酮 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 ✔ 99%
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 HCl ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

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

NCX, IC50: 33 nM

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

Calcium channel, Ki: 68 nM

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

L-type Cav1.2, IC50: 10 nM

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

Calcium channel, IC50: 2.6 nM

 		99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

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

Calcium channel, IC50: 0.03 nM

 		95%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 99%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

 		95%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 99%
Cinepazide Maleate ✔ 99% (HPLC)
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Amiloride HCl ✔ 98%
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/硫氮酮 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/硫氮酮 细胞实验

Cell Line
Concentration Treated Time Description References
MDA-MB-231 cells 1-100 μM 10 days Diltiazem significantly reduced colony formation in MDA-MB-231 cells, with 100 μM treatment reducing colony formation to 0.22±0.05-fold of control. Oncogenesis. 2022 Aug 13;11(1):48.
4T1 cells 1-100 μM 10 days Diltiazem significantly reduced colony formation in 4T1 cells, with 100 μM treatment reducing colony formation to 0.33±0.08-fold of control. Oncogenesis. 2022 Aug 13;11(1):48.
JC cells 1-100 μM 10 days Diltiazem significantly reduced colony formation in JC cells, with 100 μM treatment reducing colony formation to 0.23±0.05-fold of control. Oncogenesis. 2022 Aug 13;11(1):48.
cardiomyocytes 1 μM 5 min To evaluate the effect of Diltiazem on contractile function and calcium transients in cardiomyocytes. Results showed that Diltiazem improved diastolic function and reduced arrhythmia incidence in KI cardiomyocytes under stress conditions. J Physiol. 2017 Jun 15;595(12):3987-3999.
cardiac myocytes 10 μM To evaluate the effect of Diltiazem on mitochondrial membrane potential, results showed that Diltiazem attenuated the BayK(-)-induced increase in mitochondrial membrane potential JACC Basic Transl Sci. 2016 Feb 13;1(1-2):61-72.

(+)-cis-Diltiazem HCl/硫氮酮 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice 4T1-luc breast cancer lung metastasis model Oral gavage 1-3 mg/kg Once daily, 5 days a week for 30 days Diltiazem significantly reduced lung metastasis and nodule formation of 4T1-luc cells and increased GDF-15 expression. Oncogenesis. 2022 Aug 13;11(1):48.
New Zealand white rabbits Hypertensive model Transdermal administration 30 mg 24 hours To evaluate the antihypertensive effect of Diltiazem HCl transdermal patch, results showed sustained reduction in arterial blood pressure J Adv Res. 2016 May;7(3):539-50
Male Albino Swiss mice Mybpc3-targeted knock-in mouse model Drinking water 25 mg/kg Once daily for 6 months To evaluate the effect of long-term Diltiazem treatment on the cardiac phenotype of KI mice. Results showed that long-term Diltiazem treatment did not reverse cardiac hypertrophy, dysfunction, activation of the fetal gene program, or fibrosis. J Physiol. 2017 Jun 15;595(12):3987-3999.
Mice Transgenic mouse models of cTnT R92L and R92W Drinking water 1.8 mg Continued for three months, with treatment water changed every two days. To evaluate the effects of Diltiazem-HCl on improving diastolic function. Results showed that Diltiazem-HCl treatment arrested diastolic dysfunction progression in R92W animals only, with no improvement in cardiac remodeling in either genotype. Circulation. 2019 Mar 19;139(12):1517-1529
Mice Primary hyperparathyroidism model Oral 100mg/kg Daily administration for 2 weeks Diltiazem prevents cPTH-induced bone loss by inhibiting Th17 cell expansion and bone resorption. Cell Metab. 2015 Nov 3;22(5):799-810

(+)-cis-Diltiazem HCl/硫氮酮 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/硫氮酮 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/硫氮酮 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/硫氮酮 技术信息

CAS号33286-22-5
分子式C22H27ClN2O4S
分子量 450.98
SMILES Code CC(O[C@H]1C(N(CCN(C)C)C2=CC=CC=C2S[C@H]1C3=CC=C(OC)C=C3)=O)=O.[H]Cl
MDL No. MFCD00069252
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
InChI Key HDRXZJPWHTXQRI-BHDTVMLSSA-N
Pubchem ID 62920
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

H2O: 30 mg/mL(66.52 mM)，配合低频超声助溶

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

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/硫氮酮 纯度/质量文件 | (+)-cis-Diltiazem HCl/硫氮酮 亚型比较 | (+)-cis-Diltiazem HCl/硫氮酮 生物活性 | (+)-cis-Diltiazem HCl/硫氮酮 临床数据 | (+)-cis-Diltiazem HCl/硫氮酮 参考文献 | (+)-cis-Diltiazem HCl/硫氮酮 实验方案 | (+)-cis-Diltiazem HCl/硫氮酮 技术信息

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