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硝苯吡啶.

(Synonyms: 硝苯地平; BAY-a-1040)
目录号: PC21356 纯度: BR,98%
硝苯地平 Nifedipine (BAY-a-1040) 是有效的钙离子通道 (calcium channel) 阻滞剂,常用于心肌功能不全的相关研究。
CAS No. :21829-25-4
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中文名称
硝苯吡啶.
中文别名
硝苯地平;1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二羧酸二甲酯;心痛定;利心平;硝苯吡啶;硝苯啶;硝基地平;硝苯地平(心痛定);硝苯地平 GMP;Nifedipine 硝苯地平;长效冠脉扩张药硝苯地平;磷酸肌酸钠;硝苯地平 EP标准品;硝苯地平 USP标准品;硝苯地平 标准品;硝苯地平-D6;硝苯地平长效冠脉扩张药;硝苯地平欢迎来电洽谈;硝苯地平杂质
英文名称
Nifedipine
英文别名
Nifedipine;1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylicaciddime;3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, dimethyl ester;4-(2’-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsaeuredimethy;5-pyridinedicarboxylicacid,1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-dim;Adalat CC;bay1040;corinfar;Dimethyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate;ALDIPIN ANIFED;Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate;dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;nifedipin;Nifedipine (BAY 1040, Cordipin, Adalat®, Nifediac®, Nifedical®, Procardia®, Afeditab® );1,4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic Acid Dimethyl Ester;4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbmethoxy-1,4-dihydropyridine;Adalat;Cordipin;Fenihidin;Fenihidine;Procardia;Procardia XL;Dimethyl 1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-3,5-pyridinedicarboxylate;Oxcord;Citilat;Adalate;Nifediac;Afeditab CR;Hexadilat;Tibricol;Nifangin;Kordafen;Nifedical;Introcar;Coracten;Pidilat;Zenusin;Adapine;Sepamit;Anifed;Orix;Adalat LA;Nifedipinum;Dignokonstant;Chronadalate;Nifelat;Nifedin;Nifedicor;Nifecard;Megalat;Macorel;Fenamon;Corotrend;Cordicant;Cordafen;Nifedipino;Ecodipin
Cas No.
21829-25-4
分子式
C17H18N2O6
分子量
346.33
包装储存

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

Nifedipine (BAY-a-1040) is a potent calcium channel blocker and drug of choice for cardiac insufficiencies.

性状

Solid

体外研究(In Vitro)

Nifedipine (BAY-a-1040) (100 μM) significantly lowers the viability of the WKPT-0293 Cl.2 Cells, and treatment of nifedipine (10 or 100 μM) plus FAC induces a significant reduction in cell viability, but there are no significant differences in viability between the control cells and the cells treated with 100 μM of FAC or 1 and 10 μM of nifedipine.Nifedipine (BAY-a-1040) (1, 10, or 100 μM) significantly increases iron level in WKPT-0293 Cl.2 cells. Nifedipine treatment also increases expression of TfR1, DMT1+IRE and DMT1-IRE in WKPT-0293 Cl.2 cells. In addition, co-treatment with nifedipine (100 μM) and FAC (100 μM) increases TfR1, DMT1+IRE and DMT1-IRE expression in WKPT-0293 Cl.2 cells. Nifedipine plus ritodrine produces a significantly greater inhibition of contractility than each drug alone in the midrange of concentrations. The combination of nifedipine plus nitroglycerin or nifedipine plus atosiban produces a significantly greater inhibition than nitroglycerin or atosiban alone but not greater than nifedipine. The combination of nifedipine plus NS-1619 (Ca-activated K [BKCa] channel opener) reduces the inhibitory effect of each drug. Nifedipine (BAY-a-1040) (2 μM) significantly inhibits P. capsici mycelial growth and sporulation. Nifedipine (BAY-a-1040)-induced inhibition of mycelial growth is calcium-dependent. Nifedipine (0.5 μM) increases P. capsici sensitivity to H2O2 in a calcium-dependent manner. Nifedipine inhibition of P. capsici virulence and expression of genes involved in pathogenicity.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In Nifedipine (BAY-a-1040) (50 mg/kg)- and CsA-treated rats, the BL dimensions (BLi and BLk), MD dimensions (MDk) and vertical dimensions (VHi and VHk) are significantly increased (P < 0.05) at the end of the 4th week.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (288.74 mM; Need ultrasonic)

H2O : 1 mg/mL (2.89 mM; ultrasonic and warming and heat to 80°C)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8874 mL 14.4371 mL 28.8742 mL
5 mM 0.5775 mL 2.8874 mL 5.7748 mL
10 mM 0.2887 mL 1.4437 mL 2.8874 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.22 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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