2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Calcium Channel Reactive Oxygen Species (ROS)
  4. Nisoldipine

ニソルジピン  (Synonyms: Nisoldipine; BAY-k 5552)

製品番号: HY-17402 純度: 99.56%
COA 取扱説明書 Technical Support

Nisoldipine (BAY-k 5552; Sular) is an orally active and blood-brain barrier-penetrating dihydropyridine calcium antagonist, with greater vascular selectivity than other calcium channel antagonists. Nisoldipine inhibits calcium influx and blocks voltage-gated calcium channels. Nisoldipine dilates coronary and systemic arteries. Nisoldipine has antihypertensive and anti-anginal activity. Nisoldipine also displays neuroprotective and antiviral activity.

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Nisoldipine

ニソルジピン 構造式

CAS 番号 : 63675-72-9

容量 価格（税別） 在庫状況 数量
100 mg $35 在庫あり
500 mg $56 在庫あり
1 g $87 在庫あり
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10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Other Forms of Nisoldipine:

ニソルジピン 関連抗体

Top Publications Citing Use of Products

Calcium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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製品説明

Nisoldipine (BAY-k 5552; Sular) is an orally active and blood-brain barrier-penetrating dihydropyridine calcium antagonist, with greater vascular selectivity than other calcium channel antagonists. Nisoldipine inhibits calcium influx and blocks voltage-gated calcium channels. Nisoldipine dilates coronary and systemic arteries. Nisoldipine has antihypertensive and anti-anginal activity. Nisoldipine also displays neuroprotective and antiviral activity[1][2][7][11].

IC50 & Target

L-type calcium channel

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.003 3
Compound: Nisoldipine
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]
CHO IC50
0.003 3
Compound: Nisoldipine
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]
HepG2 EC50
10 3
Compound: Nisoldipine
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
HepG2 EC50
12.6 3
Compound: Nisoldipine
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
[PMID: 20966043]
HepG2 EC50
31.6 3
Compound: Nisoldipine
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
HepG2 EC50
10 3
Compound: Nisoldipine
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
LLC-PK1 IC50
44.1 3
Compound: Nisoldipine
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
[PMID: 12128170]
HepG2 EC50
12.6 3
Compound: Nisoldipine
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
[PMID: 20966043]
Ventricular myocyte IC50
0.08 3
Compound: Nisoldipine
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]
HepG2 EC50
31.6 3
Compound: Nisoldipine
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
Ventricular myocyte IC50
0.73 3
Compound: Nisoldipine
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]
LLC-PK1 IC50
44.1 3
Compound: Nisoldipine
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
[PMID: 12128170]
Ventricular myocyte IC50
0.08 3
Compound: Nisoldipine
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
0.73 3
Compound: Nisoldipine
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]
体外実験

Nisoldipine noncompetitively reduces the activity of human Paraoxonase 1, with an IC50 of 13.987 μM[3].
Nisoldipine (10-100 μM, 8-10 min) is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca2+ channels in fully polarised guinea-pig ventricular myocytes[4].
Nisoldipine also displays antioxidant potency with IC50 of 28.2 μM both before and after the addition of active oxygen[5].
Nisoldipine (1 μM, 90 s) largely prevents the elevation in [Ca2+]i caused by Lipopolysaccharide in Kupffer cells[6].
Nisoldipine (20 μM, 3 h pretreatment) exerts antiviral effect by interfering with the internalization of influenza A virus into A549 cells[7].
Nisoldipine (a cumulative manner from 1 to 10 and 100 nM at 5-min intervals) decreases elevated coronary perfusion pressure in NG-nitro-L-arginine (HY-12115)-perfused rat hearts[8].

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

ニソルジピン 関連抗体
体内実験

Nisoldipine (10 ppm, intragastric feeding, 4 weeks) prevents alcoholic hepatitis caused by chronic intragastric ethanol exposure in the rat, possibly by inhibition of endotoxin-mediated Kupffer cell activation[1].
Nisoldipine (1000 ppm, diet, 12-14 weeks) prevents the development of hypertension and attenuates concomitant cardiac and aortic hypertrophy in spontaneously hypertensive rats[9].
Nisoldipine (1000 ppm, diet, 22 weeks) attenuates hypertension and protects the heart, reducing the incidence of microscopic scarring, reactive interstitial and perivascular fibrosis in spontaneously hypertensive rats[10].
Nisoldipine (20-40 mg/kg, intragastric gavage, daily, from day 2 to day 21) attenuates foot-shock-induced post-traumatic stress disorder and restores normal corticosterone levels in mice[11].

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

Animal Model: Male Wistar rats with chronic intragastric ethanol exposure[1]
Dosage: 10 ppm
Administration: Added to the diet, 4 weeks
Result: Decreased serum aspartate transaminase (AST) levels, reaching 101 U/L.
Decreased steatosis and necrosis.
Blocked the swift increase in alcohol metabolism and elevated oxygen consumption in perfused livers from rats treated with alcohol.
臨床実験
分子量

388.41

分子式

C20H24N2O6
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

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

DMSO : 100 mg/mL (257.46 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 2.5746 mL 12.8730 mL 25.7460 mL
5 mM 0.5149 mL 2.5746 mL 5.1492 mL
10 mM 0.2575 mL 1.2873 mL 2.5746 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (6.44 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.44 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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, 6 months; -20°C, 1 month (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.
純度とドキュメンテーション
参考文献

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5746 mL 12.8730 mL 25.7460 mL 64.3650 mL
5 mM 0.5149 mL 2.5746 mL 5.1492 mL 12.8730 mL
10 mM 0.2575 mL 1.2873 mL 2.5746 mL 6.4365 mL
15 mM 0.1716 mL 0.8582 mL 1.7164 mL 4.2910 mL
20 mM 0.1287 mL 0.6436 mL 1.2873 mL 3.2182 mL
25 mM 0.1030 mL 0.5149 mL 1.0298 mL 2.5746 mL
30 mM 0.0858 mL 0.4291 mL 0.8582 mL 2.1455 mL
40 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6091 mL
50 mM 0.0515 mL 0.2575 mL 0.5149 mL 1.2873 mL
60 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0727 mL
80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8046 mL
100 mM 0.0257 mL 0.1287 mL 0.2575 mL 0.6436 mL
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Nisoldipine Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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:

Nisoldipine63675-72-9BAY-k 5552Calcium ChannelReactive Oxygen Species (ROS)Ca2+ channelsCa channelsHypertensionAntihypertensiveAnti-anginalSystemic arteriesAntiviralNeuroprotective.Inhibitorinhibitorinhibit

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