Proadifen hydrochloride
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.
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- Purity: 99.95%
- CAS No.: 62-68-0
- 화학식: C23H32ClNO2
- 분자량:389.96
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Proadifen hydrochloride
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
12.6 μM
Compound: Proadifen Hydrochloride
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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
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[PMID: 20966043] |
| HepG2 | EC50 |
25.1 μM
Compound: Proadifen Hydrochloride
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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
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[PMID: 20966043] |
| HepG2 | EC50 |
35.5 μM
Compound: Proadifen Hydrochloride
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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
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[PMID: 20966043] |
| HepG2 | IC50 |
2.78 μM
Compound: 92124428
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HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
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[PMID: 22586124] |
| HepG2 | IC50 |
57 μM
Compound: 92124428
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HARVARD: Cytotoxicity in HepG2 cell line
HARVARD: Cytotoxicity in HepG2 cell line
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[PMID: 22586124] |
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.
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Cell Line:A2780 and A2780cis ovarian cancer cells
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Concentration:11.09-79.86 μM
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Incubation Time:24 h and 48 h
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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.
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Cell Line:A2780 and A2780cis ovarian cancer cells
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Concentration:11.09-79.86 μM
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Incubation Time:24 h and 48 h
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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.
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.
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Animal Model:Adult male Wistar rats (200-250 g)[1].
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Dosage:25 mg/kg
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Administration:i.p., three times (forty-eight, twenty-four and one hour before electrophysiological assessments)
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Result:Resulted a significant 18%-decrease in 5-HT neuronal firing activity compared to controls in rats.
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Animal Model:Pathogen-free young adult male Sprague Dawley rats weighing 300±350 g[5]
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Dosage:15 mg/kg
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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
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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
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CAS No. 62-68-0
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Appearance Solid
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분자량 389.96
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화학식 C23H32ClNO2
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Color White to light yellow
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SMILES
O=C(OCCN(CC)CC)C(CCC)(C1=CC=CC=C1)C2=CC=CC=C2.[H]Cl
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Synonyms
SKF-525A; U-5446; RP-5171
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
2022 Jun 24;7(1):190. PMID: 35739093
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (282 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
[6]. Jendželovský R, et al. Proadifen sensitizes resistant ovarian adenocarcinoma cells to cisplatin[J]. Toxicology Letters, 2016, 243: 56-66. [Content Brief]
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 |
Proadifen hydrochloride Related Classifications
HY-B1311 Related Classifications
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