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  2. Membrane Transporter/Ion Channel Neuronal Signaling Autophagy
  3. Calcium Channel Autophagy
  4. Nifedipine

Nifedipine  (Synonyms: 硝苯地平; BAY-a-1040)

目錄號: HY-B0284 純度: 99.90%
COA 產(chǎn)品使用指南

Nifedipine (BAY-a-1040) 是有效的鈣離子通道 (calcium channel) 阻滯劑，常用于心肌功能不全的相關(guān)研究。

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Nifedipine Chemical Structure

Nifedipine Chemical Structure

CAS No. : 21829-25-4

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥500
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500 mg ￥400
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1 g ￥500
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5 g ￥700
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50 g   詢價  

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Other Forms of Nifedipine:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

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

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: NIF
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
[PMID: 31673316]
Calvarial osteoblast EC50
1.54 μM
Compound: nifedipine
Induction of mineralization in mouse calvarial osteoblasts assessed as increase of mineralized nodules formation after 21 days by alizarin red-S staining based spectrophotometric analysis
Induction of mineralization in mouse calvarial osteoblasts assessed as increase of mineralized nodules formation after 21 days by alizarin red-S staining based spectrophotometric analysis
[PMID: 23214410]
CHO IC50
0.01 μM
Compound: nifedipine
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
CHO IC50
0.05 μM
Compound: Nifedipine
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HCT-116 IC50
> 100 μM
Compound: NIF
Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay
[PMID: 31673316]
HEK293 IC50
0.022 μM
Compound: Nifedipine
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
0.055 μM
Compound: Nifedipine
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
0.086 μM
Compound: Nif
Displacement of [3H]-PN200-110 from voltage-gated calcium channel subunit alpha Cav1.2a (unknown origin) expressed in HEK293 cells after 90 mins by liquid scintillation counting analysis
Displacement of [3H]-PN200-110 from voltage-gated calcium channel subunit alpha Cav1.2a (unknown origin) expressed in HEK293 cells after 90 mins by liquid scintillation counting analysis
[PMID: 23586669]
HEK-293T IC50
1.5 μM
Compound: Nifedipine
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
[PMID: 23122865]
HEK-293T IC50
46 μM
Compound: Nifedipine
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
[PMID: 23122865]
HepG2 IC50
9.4 μM
Compound: Nifedipine
Cytotoxicity against human HepG2 cells after 24 hrs by LDH release assay
Cytotoxicity against human HepG2 cells after 24 hrs by LDH release assay
[PMID: 30554954]
L929 IC50
6.1 μM
Compound: 1
Inhibition of human Kv1.5 channel expressed in mouse L929 cells by EP voltage clamp technique
Inhibition of human Kv1.5 channel expressed in mouse L929 cells by EP voltage clamp technique
[PMID: 19004630]
LLC-MK2 IC50
101.75 μM
Compound: Nifedipine
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
LLC-MK2 IC50
588.73 μM
Compound: Nifedipine
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
MCF7 IC50
> 100 μM
Compound: NIF
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
[PMID: 31673316]
MM1.S IC50
57.9 μM
Compound: NIF
Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay
[PMID: 31673316]
SH-SY5Y IC50
1.35 μM
Compound: nifedipine
Inhibition of human Cav1.3 channel in human SH-SY5Y cells assessed as 70 mM K+ induced calcium elevation compound treated 15 mins before stimulus by Fluo-4/AM assay
Inhibition of human Cav1.3 channel in human SH-SY5Y cells assessed as 70 mM K+ induced calcium elevation compound treated 15 mins before stimulus by Fluo-4/AM assay
[PMID: 24754640]
SH-SY5Y IC50
22 μM
Compound: Nifedipine
Inhibition of voltage-dependent L-type calcium channel in 70 mM K+-induced human SH-SY5Y cells assessed as blocking of depolarization-induced Ca2+ uptake by Fluo-4/AM dye based fluorescence microplate reader assay
Inhibition of voltage-dependent L-type calcium channel in 70 mM K+-induced human SH-SY5Y cells assessed as blocking of depolarization-induced Ca2+ uptake by Fluo-4/AM dye based fluorescence microplate reader assay
[PMID: 31724859]
Ventricular myocyte IC50
0.05 μM
Compound: Nifedipine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
0.26 μM
Compound: Nifedipine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
0.3 μM
Compound: Nifedipine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
體外研究
(In Vitro)

Nifedipine (BAY-a-1040) (100 μM) 顯著降低了 WKPT-0293 Cl.2 細(xì)胞的活力，Nifedipine (10 或 100 μM) 加 FAC 處理可顯著降低細(xì)胞活力，但對照細(xì)胞與用 100 μM FAC 或 1 和 10 μM Nifedipine 處理的細(xì)胞之間的活力沒有顯著差異。Nifedipine (BAY-a-1040) (1、10 或 100 μM) 顯著提高 WKPT-0293 Cl.2 細(xì)胞中的鐵含量。Nifedipine 處理還會增加 WKPT-0293 Cl.2 細(xì)胞中 TfR1、DMT1+IRE 和 DMT1-IRE 的表達。此外，Nifedipine (100 μM) 和 FAC (100 μM) 聯(lián)合治療可增加 WKPT-0293 Cl.2 細(xì)胞中的 TfR1、DMT1+IRE 和 DMT1-IRE 表達[2]。
Nifedipine 和利托君在中等濃度范圍內(nèi)產(chǎn)生的收縮力抑制作用顯著強于單獨使用每種藥物。Nifedipine 和硝酸甘油或 Nifedipine加阿托西班的組合產(chǎn)生的抑制作用顯著強于單獨使用硝酸甘油或阿托西班，但不大于 Nifedipine。Nifedipine 加 NS-1619（Ca2+ 激活的 K+ [BKCa] 通道開放劑）的組合可降低每種藥物的抑制作用[3]。
Nifedipine (BAY-a-1040) (2 μM) 顯著抑制辣椒炭疽菌菌絲生長和孢子形成。Nifedipine (BAY-a-1040) 誘導(dǎo)的菌絲生長抑制是鈣依賴性的。Nifedipine (0.5 μM) 以鈣依賴性方式增加辣椒炭疽菌對 H2O2 的敏感性[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

在接受 Nifedipine (BAY-a-1040) (50 mg/kg) 和 CsA 治療的大鼠中，第 4 周結(jié)束時 BL 尺寸 (BLi 和 BLk)、MD 尺寸 (MDk) 和垂直尺寸 (VHi 和 VHk) 均顯著增加 (P < 0.05)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

346.33

Formula

C17H18N2O6
CAS 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

硝苯地平；心痛定；硝苯吡啶；硝苯啶
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (288.74 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.22 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻
Cell Assay
[2]

Cell viability is assessed using an MTT assay. Briefly, a total of 25 μL MTT (1 g/L in PBS) is added to each well before incubation is conducted at 37°C for 4 h. The assay is stopped by the addition of a 100 μL lysis buffer (20% SDS in 50% N’Ndimethylformamide, pH 4.7). Optical density (OD) is measured at the 570 nm wavelength by the use of an ELX-800 microplate assay reader and the results are expressed as a percentage of the absorbance measured in the control cells.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

All the 30 rats are randomLy distributed into three equal groups of ten animals each. Group 1 (control) receive olive oil for the 8 weeks. Group 2 and Group 3 receive a combination of CsA (30 mg/kg body weight) and Nf (50 mg/kg body weight) in olive oil for 8 weeks. In Group 3 rats, Azi (10 mg/kg body weight) is added to this regimen, in the 5th week. The total study period is 8 weeks.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8874 mL 14.4371 mL 28.8742 mL 72.1855 mL
5 mM 0.5775 mL 2.8874 mL 5.7748 mL 14.4371 mL
10 mM 0.2887 mL 1.4437 mL 2.8874 mL 7.2185 mL
15 mM 0.1925 mL 0.9625 mL 1.9249 mL 4.8124 mL
20 mM 0.1444 mL 0.7219 mL 1.4437 mL 3.6093 mL
25 mM 0.1155 mL 0.5775 mL 1.1550 mL 2.8874 mL
30 mM 0.0962 mL 0.4812 mL 0.9625 mL 2.4062 mL
40 mM 0.0722 mL 0.3609 mL 0.7219 mL 1.8046 mL
50 mM 0.0577 mL 0.2887 mL 0.5775 mL 1.4437 mL
60 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2031 mL
80 mM 0.0361 mL 0.1805 mL 0.3609 mL 0.9023 mL
100 mM 0.0289 mL 0.1444 mL 0.2887 mL 0.7219 mL
Help & FAQs
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產(chǎn)品名稱：
Nifedipine
目錄號：
HY-B0284
需求量：