Vadadustat
Based on 9 publication(s) in Google Scholar
Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.70%
- No. CAS: 1000025-07-9
- Fòrmula: C14H11ClN2O4
- Peso molecular:306.70
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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HY-17608
DaprodustatHIF-PH Inhibitor -
HY-13426
RoxadustatHIF-PH Inhibitor -
HY-12654
MolidustatHypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor -
HY-103227
DesidustatHIF Hydroxylase Inhibitor -
HY-109057
Enarodustat -
HY-125840
BelzutifanHIF-2α Inhibitor -
HY-101023
MK-8617HIF PHD1-3 Inhibitor -
HY-12867
PT-2385HIF-2α Inhibitor -
HY-17031
SBE-β-CDExcipient -
HY-15641
FG-2216HIF-PHD2 Inhibitor -
HY-120110
IOX4PHD2 Inhibitor -
HY-18777
KC7F2HIF/HIF Prolyl-Hydroxylase Inhibitor
Publications Citing Use of MedChemExpress (MCE) Vadadustat
More- Nat Commun. 2025 Jan 24;16(1):985. [Abstract]
- Acta Pharm Sin B. 2025 Mar;15(3):1497-1513. [Abstract]
- Life Sci. 2024 Jun 1:346:122641. [Abstract]
- Cells. 2020 Nov 1;9(11):2396. [Abstract]
- J Biol Chem. 2021 Jan-Jun:296:100397. [Abstract]
- Drug Test Anal. 2025 May;17(5):647-654. [Abstract]
- Drug Test Anal. 2021 Feb;13(2):283-298. [Abstract]
- Patent. US20250262229A1.
- SSRN. 2023 Aug 15.
Customer Validation & Images
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RT-PCR
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WB
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Bio/Physico-chemical Assay
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RT-PCR
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Bio/Physico-chemical Assay
Actividad biológica
Descripciòn
IC50 & Target
IC50: HIF-PH[1]
In Vitro
Vadadustat induces endogenous erythropoietin synthesis and enhances iron mobilization[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1000025-07-9
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Appearance Solid
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Peso molecular 306.70
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Fòrmula C14H11ClN2O4
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Color White to off-white
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SMILES
O=C(O)CNC(C1=NC=C(C2=CC=CC(Cl)=C2)C=C1O)=O
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Synonyms
PG-1016548; AKB-6548
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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Nat Commun
Lysosomes finely control macrophage inflammatory function via regulating the release of lysosomal Fe2+ through TRPML1 channel. [Abstract]2025 Jan 24;16(1):985. PMID: 39856099
Vadadustat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 24;16(1):985. [Abstract]
Relative IL1B mRNA levels in BMDMs under control, ML-SA5, ML-SA5 + Roxadustat (100 μM), ML-SA5 + Vadadustat (200 μM), or ML-SA5 + GSK1278863 (250 μM). All treatments were for 24 h. n = 4–10.
Vadadustat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 24;16(1):985. [Abstract]
Representative immunoblots and quantitative analysis of pro IL-1β protein levels in BMDMs under control, LPS, LPS + ML-SA5, LPS + ML-SA5 + Roxadustat, LPS + ML-SA5 + Vadadustat, LPS + ML-SA5 + GSK1278863, Roxadustat, Vadadustat, or GSK1278863. All treatments were for 24 h. n = 3-6.
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Acta Pharm Sin B
Ginsenoside CK targets PHD2 to prevent platelet adhesion and enhance blood circulation by modifying the three-dimensional arrangement of collagen. [Abstract]2025 Mar;15(3):1497-1513. PMID: 40370536 -
Life Sci
The drug-specific properties of hypoxia-inducible factor-prolyl hydroxylase inhibitors in mice reveal a significant contribution of the kidney compared to the liver to erythropoietin induction. [Abstract]2024 Jun 1:346:122641. PMID: 38614299 -
Cells
Vadadustat, a HIF Prolyl Hydroxylase Inhibitor, Improves Immunomodulatory Properties of Human Mesenchymal Stromal Cells. [Abstract]2020 Nov 1;9(11):2396. PMID: 33139632
Vadadustat purchased from MedChemExpress. Usage Cited in: Cells. 2020 Nov 1;9(11):2396. [Abstract]
We performed real-time PCR analysis of selected genes on the 6 BM-MSCs populations incubated for 6 h under standard grown conditions (control) or with 40 μM Vadadustat.
Vadadustat purchased from MedChemExpress. Usage Cited in: Cells. 2020 Nov 1;9(11):2396. [Abstract]
The effect of Vadadustat preconditioning on BM-MSCs cytokine and chemokine secretion profile was determined after 24 h cells treatment with 40 μM Vadadustat by the antibody based Proteome profiler array.
Vadadustat purchased from MedChemExpress. Usage Cited in: Cells. 2020 Nov 1;9(11):2396. [Abstract]
MSCs preconditioning with Vadadustat resulted in a reduction of IL6 secretion from an average of 199 pg/mL to 103 pg/mL.
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J Biol Chem
Development of a colorimetric α-ketoglutarate detection assay for prolyl hydroxylase domain (PHD) proteins. [Abstract]2021 Jan-Jun:296:100397. PMID: 33571527
Vadadustat purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2021 Jan-Jun:296:100397. [Abstract]
Dose-response curve of Vadadustat generated by adding increasing concentrations of Vadadustat to 0.5 mM α-ketoglutarate, 100 μM HIF peptide, and 3 μM of PHD2. Plotted data represent three independent replicates.
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Drug Test Anal
Simultaneous detection of three hypoxia-inducible factor stabilizers-molidustat, roxadustat, and vadadustat-in multiple keratinized matrices and its application in a doping context. [Abstract]2025 May;17(5):647-654. PMID: 38992954 -
Drug Test Anal
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]2021 Feb;13(2):283-298. PMID: 32852861 -
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Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (326.05 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. 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. 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.15 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.
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: ≥ 2.5 mg/mL (8.15 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 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:
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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.
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 (272 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Pergola PE, et al. Vadadustat, a novel oral HIF stabilizer, provides effective anemia treatment in nondialysis-dependent chronic kidney disease. Kidney Int. 2016 Nov;90(5):1115-1122. [Content Brief]
[2]. Gupta N, et al. Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD. Am J Kidney Dis. 2017 Feb 24. pii: S0272-6386(17)30110-5. [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. 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 | 3.2605 mL | 16.3026 mL | 32.6052 mL | 81.5129 mL |
| 5 mM | 0.6521 mL | 3.2605 mL | 6.5210 mL | 16.3026 mL | |
| 10 mM | 0.3261 mL | 1.6303 mL | 3.2605 mL | 8.1513 mL | |
| 15 mM | 0.2174 mL | 1.0868 mL | 2.1737 mL | 5.4342 mL | |
| 20 mM | 0.1630 mL | 0.8151 mL | 1.6303 mL | 4.0756 mL | |
| 25 mM | 0.1304 mL | 0.6521 mL | 1.3042 mL | 3.2605 mL | |
| 30 mM | 0.1087 mL | 0.5434 mL | 1.0868 mL | 2.7171 mL | |
| 40 mM | 0.0815 mL | 0.4076 mL | 0.8151 mL | 2.0378 mL | |
| 50 mM | 0.0652 mL | 0.3261 mL | 0.6521 mL | 1.6303 mL | |
| 60 mM | 0.0543 mL | 0.2717 mL | 0.5434 mL | 1.3585 mL | |
| 80 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0189 mL | |
| 100 mM | 0.0326 mL | 0.1630 mL | 0.3261 mL | 0.8151 mL |
Vadadustat Related Classifications
HY-101277 Related Classifications
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