Nifedipine (Synonyms: BAY-a-1040)

Name: Nifedipine
Brand: MedChemExpress
SKU: HY-B0284
Rating: 5.0 (15 reviews)

Cat. No.: HY-B0284 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Nifedipine Chemical Structure

CAS No. : 21829-25-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
1 g	USD 66	In-stock	Estimated Time of Arrival: December 31
5 g	USD 106	In-stock	Estimated Time of Arrival: December 31
10 g	USD 132	In-stock	Estimated Time of Arrival: December 31
50 g		Get quote

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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Nifedipine:

15 Publications Citing Use of MCE Nifedipine

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

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]

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^[2]. 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 (Ca²⁺-activated K⁺ [BKCa] channel opener) reduces the inhibitory effect of each drug^[3]. 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^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

346.33

Formula

C₁₇H₁₈N₂O₆

CAS No.

21829-25-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (288.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (285 KB) SDS (419 KB)

COA (259 KB) HNMR (241 KB) RP-HPLC (243 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Ratre MS, et al. Effect of azithromycin on gingival overgrowth induced by cyclosporine A + nifedipine combination therapy: A morphometric analysis in rats. J Indian Soc Periodontol. 2016 Jul-Aug;20(4):396-401. [Content Brief]

[2]. Carvajal JA, et al. The Synergic In Vitro Tocolytic Effect of Nifedipine Plus Ritodrine on Human Myometrial Contractility. Reprod Sci. 2017 Apr;24(4):635-640. [Content Brief]

[3]. Yu SS, et al. Nifedipine Increases Iron Content in WKPT-0293 Cl.2 Cells via Up-Regulating Iron Influx Proteins. Front Pharmacol. 2017 Feb 13;8:60 [Content Brief]

[4]. Liu P, et al. The L-type Ca(2+) Channel Blocker Nifedipine Inhibits Mycelial Growth, Sporulation, and Virulence of Phytophthora capsici. Front Microbiol. 2016 Aug 4;7:1236. [Content Brief]

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.
References	[1]. Ratre MS, et al. Effect of azithromycin on gingival overgrowth induced by cyclosporine A + nifedipine combination therapy: A morphometric analysis in rats. J Indian Soc Periodontol. 2016 Jul-Aug;20(4):396-401. [Content Brief] [2]. Carvajal JA, et al. The Synergic In Vitro Tocolytic Effect of Nifedipine Plus Ritodrine on Human Myometrial Contractility. Reprod Sci. 2017 Apr;24(4):635-640. [Content Brief] [3]. Yu SS, et al. Nifedipine Increases Iron Content in WKPT-0293 Cl.2 Cells via Up-Regulating Iron Influx Proteins. Front Pharmacol. 2017 Feb 13;8:60 [Content Brief] [4]. Liu P, et al. The L-type Ca(2+) Channel Blocker Nifedipine Inhibits Mycelial Growth, Sporulation, and Virulence of Phytophthora capsici. Front Microbiol. 2016 Aug 4;7:1236. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Nifedipine Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nifedipine21829-25-4BAY-a-1040Calcium ChannelAutophagyCa2+ channelsCa channelsInhibitorinhibitorinhibit

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Nifedipine (Synonyms: BAY-a-1040)

Customer Review

Other Forms of Nifedipine:

Nifedipine Related Antibodies

15 Publications Citing Use of MCE Nifedipine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All Calcium Channel Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Nifedipine Related Antibodies

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Complete Stock Solution Preparation Table

Nifedipine Related Classifications

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