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

Isradipine  (Synonyms: PN 200-110; イスラジピン)

製品番号: HY-B0233 純度: 99.97%
COA 取扱説明書 Technical Support

Isradipine (PN 200-110) is an orally active and blood-brain barrier permeability L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.

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Isradipine

Isradipine 構造式

CAS 番号 : 75695-93-1

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 47 在庫あり
Solution
10 mM * 1 mL in DMSO USD 47 在庫あり
Solid
5 mg $43 在庫あり
10 mg $68 在庫あり
25 mg $140 在庫あり
50 mg $228 在庫あり
100 mg $372 在庫あり
200 mg   お問い合わせ  
500 mg   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

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Based on 0 publication(s) in Google Scholar

Other Forms of Isradipine:

Isradipine 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

Isradipine (PN 200-110) is an orally active and blood-brain barrier permeability L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3].

IC50 & Target

L-type calcium channel

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.0022 μM
Compound: Isradipine
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
0.107 μM
Compound: Isradipine
Antagonist activity at rabbit voltage-dependent L-type calcium channel Cav1.2alpha-1C expressed in HEK293 cells by FLIPR assay
Antagonist activity at rabbit voltage-dependent L-type calcium channel Cav1.2alpha-1C expressed in HEK293 cells by FLIPR assay
[PMID: 23688558]
HEK293 IC50
0.221 μM
Compound: Isradipine
Antagonist activity at rat voltage-dependent L-type calcium channel Cav1.3alpha-1D expressed in HEK293 cells by FLIPR assay
Antagonist activity at rat voltage-dependent L-type calcium channel Cav1.3alpha-1D expressed in HEK293 cells by FLIPR assay
[PMID: 23688558]
体外実験

Isradipine has much higher (＞40 fold) affinity for Cav1.3 channels as well as good brain bioavailability. Isradipine has nearly equal potency at Cav1.2 and Cav1.3 channels[1].

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

Isradipine 関連抗体
体内実験

Isradipine (0.1~3 mg/kg; p.o.) makes sodium excretion increase in a dose-dependent manner[3].
Isradipine pre-treatment reduces 6-hydroxydopamine induced neurotoxicity at the striatal level. Protective effect of isradipine at the striatal level is dose-dependent as shown from 6 mice. Isradipine pre-treatment increases the number of surviving SNc DA cells after 6-hydroxydopamine induced degeneration. Isradipine is capable of protecting striatal dopaminergic terminals and SNc dopaminergic cell bodies against a slow, progressive insult created by intrastriatal injection of 6-hydroxydopamine[1].

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

Animal Model: Rats[3]
Dosage: 0.1~3 mg/kg
Administration: P.o.
Result: Sodium excretion increased in a dose-dependent manner.  
臨床実験
分子量

371.39

分子式

C19H21N3O5
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C)NC(C)=C(C(OC(C)C)=O)C1C2=CC=CC3=NON=C23)OC
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (269.26 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6926 mL 13.4629 mL 26.9259 mL
5 mM 0.5385 mL 2.6926 mL 5.3852 mL
10 mM 0.2693 mL 1.3463 mL 2.6926 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 (6.73 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 (6.73 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).
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

純度: 99.97%

COA (254 KB) LCMS (96 KB)

取扱説明書 (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6926 mL 13.4629 mL 26.9259 mL 67.3147 mL
5 mM 0.5385 mL 2.6926 mL 5.3852 mL 13.4629 mL
10 mM 0.2693 mL 1.3463 mL 2.6926 mL 6.7315 mL
15 mM 0.1795 mL 0.8975 mL 1.7951 mL 4.4876 mL
20 mM 0.1346 mL 0.6731 mL 1.3463 mL 3.3657 mL
25 mM 0.1077 mL 0.5385 mL 1.0770 mL 2.6926 mL
30 mM 0.0898 mL 0.4488 mL 0.8975 mL 2.2438 mL
40 mM 0.0673 mL 0.3366 mL 0.6731 mL 1.6829 mL
50 mM 0.0539 mL 0.2693 mL 0.5385 mL 1.3463 mL
60 mM 0.0449 mL 0.2244 mL 0.4488 mL 1.1219 mL
80 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8414 mL
100 mM 0.0269 mL 0.1346 mL 0.2693 mL 0.6731 mL
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Isradipine 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:

Isradipine75695-93-1PN 200-110Calcium ChannelAutophagyCa2+ channelsCa channelsL-typecalciumchannelpowerfulperipheralvasodilatordihydropyridineselective peripheralcirculationneuroprotectiveParkinson'sInhibitorinhibitorinhibit

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製品番号:
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