Art. -Nr.: HY-101277

Vadadustat

(Synonyms: PG-1016548; AKB-6548)

9 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.70%
CAS. Nr.: 1000025-07-9
Formel: C₁₄H₁₁ClN₂O₄
Molecular Weight:306.70

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Vadadustat Chemical Structure

CAS. Nr.: 1000025-07-9

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor^[1]. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo^[1]^[2].

IC₅₀ & Target

IC50: HIF-PH^[1]

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1000025-07-9
Appearance Solid
Molecular Weight 306.70
Formel C₁₄H₁₁ClN₂O₄
Color White to off-white
SMILES

O=C(O)CNC(C1=NC=C(C2=CC=CC(Cl)=C2)C=C1O)=O
Synonyms

PG-1016548; AKB-6548
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (9)

All Bio/Physico-chemical AssayRT-PCRWB

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Journal Impact Factor

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.
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
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.
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
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.
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
Patent

US20250262229A1.
SSRN

2023 Aug 15.

Lösungsmittel & Löslichkeit

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)

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

3.2605 mL

16.3026 mL

32.6051 mL

5 mM

0.6521 mL

3.2605 mL

6.5210 mL

10 mM

0.3261 mL

1.6303 mL

3.2605 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. 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: ≥ 2.5 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (8.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (272 KB)
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)
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]. 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]

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

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
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

Keywords

Vadadustat

9 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Vadadustat

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vadadustat Related Classifications

HY-101277 Related Classifications