2. Metabolic Enzyme/Protease Neuronal Signaling Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Cytochrome P450 Monoamine Oxidase Bcl-2 Family Survivin PARP
  4. Proadifen hydrochloride

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

Cat. No.: HY-B1311 Purity: 99.98%
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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.

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

Proadifen hydrochloride Chemical Structure

Proadifen hydrochloride Chemical Structure

CAS No. : 62-68-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Proadifen hydrochloride:

Proadifen hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Proadifen hydrochloride

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

View All Monoamine Oxidase Isoform Specific Products:

View All Isoforms
MAO-A MAO-B

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5][6].

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]
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.

Proadifen hydrochloride Related Antibodies

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.
Molecular Weight

389.96

Formula

C23H32ClNO2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5644 mL 12.8218 mL 25.6437 mL
5 mM 0.5129 mL 2.5644 mL 5.1287 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 (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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 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.

    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: ≥ 2.08 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.

    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 (sealed storage, away from moisture)

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: 99.98%

SDS (252 KB)

COA (251 KB) HNMR (207 KB) LCMS (114 KB)

Handling Instructions (2659 KB)
References

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 (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.

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
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Proadifen hydrochloride Related Classifications

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  • 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:

Proadifen62-68-0SKF-525A U-5446 RP-5171U5446U 5446U-5446RP5171RP 5171RP-5171Cytochrome P450Monoamine OxidaseBcl-2 FamilySurvivinPARPCYPsMAOpoly ADP ribose polymeraseCytochrome P450 inhibitormonoamine oxidase AantidepressantDMTliver microsomesAcridoneprostaglandin E2ratayahuascainflammationovarian carcinomaInhibitorinhibitorinhibit

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