Art. -Nr.: HY-B1311

Proadifen hydrochloride

(Synonyms: SKF-525A; U-5446; RP-5171)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC₅₀ value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.95%
CAS. Nr.: 62-68-0
Formel: C₂₃H₃₂ClNO₂
Molecular Weight:389.96

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Proadifen hydrochloride Chemical Structure

CAS. Nr.: 62-68-0

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen :

MAO-A
MAO-B

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	12.6 μM Compound: Proadifen Hydrochloride	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	25.1 μM Compound: Proadifen Hydrochloride	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	35.5 μM Compound: Proadifen Hydrochloride	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	IC₅₀	2.78 μM Compound: 92124428	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	[PMID: 22586124]
HepG2	IC₅₀	57 μM Compound: 92124428	HARVARD: Cytotoxicity in HepG2 cell line HARVARD: Cytotoxicity in HepG2 cell line	[PMID: 22586124]

In Vitro

Proadifen hydrochloride (10 mM, 60 min) has a larger inhibition on N, N-dimethyltryptamine (DMT) metabolism compared to Quinidine (HY-B1751H) (2.1-fold increase in half-life) in liver microsomes^[2].
Proadifen hydrochloride (8 μM, 2 min) inhibits the formation of Acridone (HY-W007771) with 50% inhibition in rat hepatic cytosolic fraction^[3].
Proadifen hydrochloride (11.09-79.86 μM, 24 h and 48 h) combined with Cisplatin (CDDP) (HY-17394) inhibits cell proliferation, metabolic activity, the upregulation of MRP1, MRP2, CYP3A4 proteins levels induced by CDDP (HY-17394) and attenuates cell cycle arrest, also downregulates the expression of Bcl-XL, Bcl-2, survivin, but increases PARP cleavage in A2780 and A2780cis ovarian cancer cells^[6].

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

Cell Cycle Analysis^[6]

Cell Line:

A2780 and A2780cis ovarian cancer cells
Concentration:

11.09-79.86 μM
Incubation Time:

24 h and 48 h
Result:

Significantly attenuated CDDP (HY-17394)-mediated S-phase arrest and increased accumulation of A2780cis cells in the G0/G1 phase in A2780 and A2780cis ovarian cancer cells.

Western Blot Analysis^[6]

Cell Line:

A2780 and A2780cis ovarian cancer cells
Concentration:

11.09-79.86 μM
Incubation Time:

24 h and 48 h
Result:

Reduced the levels of the MRP1, MRP2, CYP3A4, BCRP proteins levels and downregulated the expression of Bcl-XL, Bcl-2, survivin, but increased PARP cleavage combined with CDDP (HY-17394) in A2780 and A2780cis cells.

In Vivo

Proadifen hydrochloride (25 mg/kg, i.p., three times) inhibits the excitability of 5-HT neurons, Corticosterone (HY-B1618) might play a key role in the Proadifen hydrochloride-induced inhibition of 5-HT neurons in rats^[1]^[4].
Proadifen hydrochloride (15 mg/kg, i.p., a single dose for 3 h) exacerbates PGE2 levels elevated by LPS in rats^[5].

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

Animal Model:

Adult male Wistar rats (200-250 g)^[1].
Dosage:

25 mg/kg
Administration:

i.p., three times (forty-eight, twenty-four and one hour before electrophysiological assessments)
Result:

Resulted a significant 18%-decrease in 5-HT neuronal firing activity compared to controls in rats.

Animal Model:

Pathogen-free young adult male Sprague Dawley rats weighing 300±350 g^[5]
Dosage:

15 mg/kg
Administration:

i.m. or i.p., injected i.p. with LPS (50 mg/kg) after pretreated i.m. Proadifen hydrochloride for 1 h lasting 8 h or 30 min lasting 3 h
Result:

Significantly augmented Lipopolysaccharide (LPS)-induced fever in rats.
Induced an even larger elevation of PGE2 in LPS injected rats to 343.4245.4 pg/mL in rats.

Chemical Information

CAS. Nr. 62-68-0
Appearance Solid
Molecular Weight 389.96
Formel C₂₃H₃₂ClNO₂
Color White to light yellow
SMILES

O=C(OCCN(CC)CC)C(CCC)(C1=CC=CC=C1)C2=CC=CC=C2.[H]Cl
Synonyms

SKF-525A; U-5446; RP-5171
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (1)

All

Sort by:

Journal Impact Factor

Signal Transduct Target Ther

CB1R-stabilized NLRP3 inflammasome drives antipsychotics cardiotoxicity. [Abstract]

2022 Jun 24;7(1):190. PMID: 35739093

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (128.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.5644 mL

12.8218 mL

25.6437 mL

5 mM

0.5129 mL

2.5644 mL

5.1287 mL

10 mM

0.2564 mL

1.2822 mL

2.5644 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.08 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

Verweise

[1]. Grinchii D, et al. Inhibition of cytochrome P450 by proadifen diminishes the excitability of brain serotonin neurons in rats[J]. Gen Physiol Biophys. 2018 Sep;37(6):711-713. [Content Brief]

[2]. Eckernäs E, et al. N, N-dimethyltryptamine forms oxygenated metabolites via CYP2D6 - an in vitro investigation[J]. Xenobiotica. 2023 Dec;53(8-9):515-522. [Content Brief]

[3]. Robertson IG, et al. Inhibition by SKF-525A of the aldehyde oxidase-mediated metabolism of the experimental antitumour agent acridine carboxamide[J]. Biochem Pharmacol. 1993 May 25;45(10):2159-62. [Content Brief]

[4]. Paliokha R, et al. Inhibition of cytochrome P450 with proadifen alters the excitability of brain catecholamine-secreting neurons[J]. Gen Physiol Biophys. 2022 May;41(3):255-262. [Content Brief]

[5]. Kozak W, et al. Proadifen (SKF-525A), an inhibitor of cytochrome P-450, augments LPS-induced fever and exacerbates prostaglandin-E2 levels in the rat[J]. Journal of Thermal Biology, 2000, 25(1-2): 45-50.

[6]. Jendželovský R, et al. Proadifen sensitizes resistant ovarian adenocarcinoma cells to cisplatin[J]. Toxicology Letters, 2016, 243: 56-66. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5644 mL	12.8218 mL	25.6437 mL	64.1091 mL
	5 mM	0.5129 mL	2.5644 mL	5.1287 mL	12.8218 mL
	10 mM	0.2564 mL	1.2822 mL	2.5644 mL	6.4109 mL
	15 mM	0.1710 mL	0.8548 mL	1.7096 mL	4.2739 mL
	20 mM	0.1282 mL	0.6411 mL	1.2822 mL	3.2055 mL
	25 mM	0.1026 mL	0.5129 mL	1.0257 mL	2.5644 mL
	30 mM	0.0855 mL	0.4274 mL	0.8548 mL	2.1370 mL
	40 mM	0.0641 mL	0.3205 mL	0.6411 mL	1.6027 mL
	50 mM	0.0513 mL	0.2564 mL	0.5129 mL	1.2822 mL
	60 mM	0.0427 mL	0.2137 mL	0.4274 mL	1.0685 mL
	80 mM	0.0321 mL	0.1603 mL	0.3205 mL	0.8014 mL
	100 mM	0.0256 mL	0.1282 mL	0.2564 mL	0.6411 mL

Proadifen hydrochloride

1 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Proadifen hydrochloride

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Mitochondria-Targeted Compound Library

Antidepressant Compound Library

Metabolic Enzyme Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Proadifen hydrochloride

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Proadifen hydrochloride Related Classifications

HY-B1311 Related Classifications