Pyridoxal isonicotinoyl hydrazone
Based on 4 publication(s) in Google Scholar
Pyridoxal isonicotinoyl hydrazone is an orally active and lipophilic iron-specific chelator that acts as a non-competitive inhibitor of ferrochelatase (FECH) by binding iron ions. Pyridoxal isonicotinoyl hydrazone disrupts heme biosynthesis, leading to reduced FECH stability and increased protoporphyrin IX (PPIX) accumulation. Pyridoxal isonicotinoyl hydrazone is promising for research of iron-overload diseases (e.g., β-thalassemia).
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- Pureza: 99.96%
- No. CAS: 737-86-0
- Fòrmula: C14H14N4O3
- Peso molecular:286.29
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Pyridoxal isonicotinoyl hydrazone
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Actividad biológica
Pyridoxal isonicotinoyl hydrazone (50-800 µM; 24-72 h) decreases FECH protein levels without affecting FECH mRNA, accompanied by increased ALAS1 protein at high doses in primary human hepatocytes (PHHs) and HepG2/C3A cells[3].
Pyridoxal isonicotinoyl hydrazone (50 µM; 24 h) reduces FECH protein by 40%, an effect reversed by iron supplementation in HepG2/C3A cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats
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Dosage:100, 400, 800 mg/kg (dissolved in distilled water)
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Administration:Oral gavage, daily for 90 days
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Result:Significant increased the serum alkaline phosphatase (+30%), SGOT (+18%), and SGPT (+20%) at 800 mg/kg at week 13, with hepatic vacuolization, nuclear degeneration, and renal/spleen vascular congestion.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 737-86-0
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Appearance Solid
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Peso molecular 286.29
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Fòrmula C14H14N4O3
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Color Light yellow to yellow
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SMILES
CC1=NC=C(C(/C=N/NC(C2=CC=NC=C2)=O)=C1O)CO
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Mammalian SLC39A13 promotes ER/Golgi iron transport and iron homeostasis in multiple compartments. [Abstract]2024 Dec 30;15(1):10838. PMID: 39738060 -
J Pharm Anal
Hydralazine represses Fpn ubiquitination to rescue injured neurons via competitive binding to UBA52. [Abstract]2024 Jan;14(1):86-99. PMID: 38352945 -
Commun Biol
FGFR1 governs iron homeostasis via regulating intracellular protein degradation pathways of IRP2 in prostate cancer cells. [Abstract]2024 Aug 17;7(1):1011. PMID: 39154074 -
Biomed Res Int
Pyridoxal Isonicotinoyl Hydrazone Improves Neurological Recovery by Attenuating Ferroptosis and Inflammation in Cerebral Hemorrhagic Mice. [Abstract]2021 Sep 8;2021:9916328. PMID: 34541001
Solvente y solubilidad
DMSO : 7 mg/mL (24.45 mM; ultrasonic and heat to 60°C; 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 (protect from light). 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 (protect from light). 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: ≥ 1.47 mg/mL (5.13 mM); Clear solution
This protocol yields a clear solution of ≥ 1.47 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.7 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: ≥ 1.47 mg/mL (5.13 mM); Clear solution
This protocol yields a clear solution of ≥ 1.47 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.7 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 (protect from light)
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hermes-Lima M, et al. The iron chelator pyridoxal isonicotinoyl hydrazone (PIH) and its analogues prevent damage to 2-deoxyribose mediated by ferric iron plus ascorbate. Biochim Biophys Acta. 2000 Oct 18;1523(2-3):154-60. [Content Brief]
[2]. Landschulz W, et al. A lipophilic iron chelator can replace transferrin as a stimulator of cell proliferation and differentiation. J Cell Biol. 1984 Feb;98(2):596-601. [Content Brief]
[3]. Brewer CT, et al. The Isoniazid Metabolites Hydrazine and Pyridoxal Isonicotinoyl Hydrazone Modulate Heme Biosynthesis. Toxicol Sci. 2019 Mar 1;168(1):209-224. [Content Brief]
[4]. Sookvanichsilp N, et al. Toxicological study of pyridoxal isonicotinoyl hydrazone: acute and subchronic toxicity. Drug Chem Toxicol. 1991;14(4):395-403. [Content Brief]
[5]. Buss JL, et al. Oxidative stress mediates toxicity of pyridoxal isonicotinoyl hydrazone analogs. Arch Biochem Biophys. 2004 Jan 1;421(1):1-9. [Content Brief]
[6]. Zhang H, et al. Pyridoxal Isonicotinoyl Hydrazone Improves Neurological Recovery by Attenuating Ferroptosis and Inflammation in Cerebral Hemorrhagic Mice. Biomed Res Int. 2021 Sep 8;2021:9916328. [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 (protect from light). 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 |
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| DMSO | 1 mM | 3.4930 mL | 17.4648 mL | 34.9296 mL | 87.3240 mL |
| 5 mM | 0.6986 mL | 3.4930 mL | 6.9859 mL | 17.4648 mL | |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.4930 mL | 8.7324 mL | |
| 15 mM | 0.2329 mL | 1.1643 mL | 2.3286 mL | 5.8216 mL | |
| 20 mM | 0.1746 mL | 0.8732 mL | 1.7465 mL | 4.3662 mL |
Pyridoxal isonicotinoyl hydrazone Related Classifications
HY-114758 Related Classifications
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