Cat. No.: HY-B0347

Lacidipine

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).

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Pureté: 99.40%
CAS No.: 103890-78-4
Formule: C₂₆H₃₃NO₆
Masse moléculaire:455.54

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Lacidipine Chemical Structure

CAS No.: 103890-78-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

L-type calcium channel

Voir tous les produits spécifiques à Isoform Calcium Channel :

Voir tous les produits spécifiques à Isoform Caspase :

In Vitro

Lacidipine (0.01-100 μM; 24 h) inhibits HKCs proliferation in vitro in a concentration-dependent manner^[1].
Lacidipine (0.01-100 μM; 24 h) protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HKC cells
Concentration:

0.01-100 μM
Incubation Time:

24 h
Result:

Exhibited anti-proliferative activity in a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

HKC cells (renal ischemia reperfusion (I/R) model)
Concentration:

1, 10 μM
Incubation Time:

24 h
Result:

AA-induced HKC cells apoptosis, with proportion of early apoptotic cells of 1.47% and 0.30% for 1 and 10 μM dosage, respectively.

Western Blot Analysis^[1]

Cell Line:

HKC cells (renal ischemia reperfusion (I/R) model)
Concentration:

1, 10 μM
Incubation Time:

24 h (pretreat)
Result:

Decreased the expression of cyt c of injured cells following ATP depletion and recovery.
Significantly increased the expression of the Bcl-2 protein, but decreased the Bax protein.

In Vivo

Lacidipine (0.3, 1.0, 3.0 mg/kg; p.o.; single daily for 10 weeks) shows anti-atherogenic effects in the apoE-deficient mouse, and reduces plasma endothelin concentrations^[2].

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

Animal Model:

Female C57BL/6 mice (Homozygous; apoE-deficient; atherosclerosis model)^[2].
Dosage:

0.3, 1.0, 3.0 mg/kg
Administration:

Oral gavage; single daily for 10 weeks.
Result:

Induced a significant dose-dependent decrease in plasma endothelin levels.
Significantly reduced the mean lesion area in a dose-related manner by 10, 17 and 53% for 0.3, 1.0, 3.0 mg/kg, respectively.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 103890-78-4
Appearance Solid
Masse moléculaire 455.54
Formule C₂₆H₃₃NO₆
Color White to off-white
SMILES

O=C(C1=C(C)NC(C)=C(C(OCC)=O)C1C2=CC=CC=C2/C=C/C(OC(C)(C)C)=O)OCC
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Sci Rep

Elucidating host cell response pathways and repurposing therapeutics for SARS-CoV-2 and other coronaviruses. [Abstract]

2022 Nov 5;12(1):18811. PMID: 36335206
University of Colorado Denver

2024.

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (109.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1952 mL

10.9760 mL

21.9520 mL

5 mM

0.4390 mL

2.1952 mL

4.3904 mL

10 mM

0.2195 mL

1.0976 mL

2.1952 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (5.49 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang A, et al. Lacidipine attenuates apoptosis via a caspase-3 dependent pathway in human kidney cells. Cell Physiol Biochem. 2013;32(4):1040-9.

[2]. Cristofori P, et al. The calcium-channel blocker lacidipine reduces the development of atherosclerotic lesions in the apoE-deficient mouse. J Hypertens. 2000 Oct;18(10):1429-36. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.1952 mL	10.9760 mL	21.9520 mL	54.8799 mL
	5 mM	0.4390 mL	2.1952 mL	4.3904 mL	10.9760 mL
	10 mM	0.2195 mL	1.0976 mL	2.1952 mL	5.4880 mL
	15 mM	0.1463 mL	0.7317 mL	1.4635 mL	3.6587 mL
	20 mM	0.1098 mL	0.5488 mL	1.0976 mL	2.7440 mL
	25 mM	0.0878 mL	0.4390 mL	0.8781 mL	2.1952 mL
	30 mM	0.0732 mL	0.3659 mL	0.7317 mL	1.8293 mL
	40 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3720 mL
	50 mM	0.0439 mL	0.2195 mL	0.4390 mL	1.0976 mL
	60 mM	0.0366 mL	0.1829 mL	0.3659 mL	0.9147 mL
	80 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6860 mL
	100 mM	0.0220 mL	0.1098 mL	0.2195 mL	0.5488 mL

Keywords

Lacidipine

2 Cited Publications

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Lacidipine

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

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Publications Citing Use of MedChemExpress (MCE) Lacidipine

Voir tous les produits spécifiques à Isoform Calcium Channel

Voir tous les produits spécifiques à Isoform Caspase

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Lacidipine Related Classifications

HY-B0347 Related Classifications