2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. Vadadustat

Vadadustat  (Synonyms: PG-1016548; AKB-6548)

Cat. No.: HY-101277 Purity: 99.51%
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Vadadustat (PG-1016548) est un inhibiteur titrable de la prolyl hydroxylase inductible par l'hypoxie orale (HIF-PH). Vadadustat est un agent l'érythropoïèse-stimulant et a le potentiel pour le traitement de l'anémie dans les maladies rénales chroniques in vivo.

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.

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

Vadadustat Chemical Structure

Vadadustat Chemical Structure

CAS No. : 1000025-07-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 130 In-stock
Solution
10 mM * 1 mL in DMSO USD 130 In-stock
Solid
2 mg USD 77 In-stock
5 mg USD 132 In-stock
10 mg USD 209 In-stock
50 mg USD 539 In-stock
100 mg USD 759 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 4 publication(s) in Google Scholar

Vadadustat Related Antibodies

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HIF-1α HIF

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Description

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]
In Vitro

Vadadustat induces endogenous erythropoietin synthesis and enhances iron mobilization. Vadadustat is well-tolerated in healthy volunteers and patients with chronic kidney disease, where it increases reticulocytes, plasma EPO, and Hb levels in a dose-dependent manner. The increase in plasma EPO levels seen with vadadustat is comparable in magnitude to that occurring physiologically at moderate altitude and shows a normal diurnal pattern with a return to baseline levels prior to the next dose. Vadadustat improves iron homeostasis by decreasing hepcidin and increasing transferrin levels. once-daily oral administration of vadadustat, titrated to increase and maintain Hb in the target range, may provide multiple advantages over conventional ESAs[1]. Vadadustat is observed to have a half-life of approximately 4.5 hours. Overall, patients demonstrate an increase in Hb levels, from 9.91 g/dL at baseline to 10.54 g/dL by day 29. Ferritin levels decrease from 334.1 ng/mL at baseline to 271.7 ng/mL by day 29[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Vadadustat Related Antibodies
Clinical Trial
Molecular Weight

306.70

Formula

C14H11ClN2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2605 mL 16.3026 mL 32.6051 mL
5 mM 0.6521 mL 3.2605 mL 6.5210 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. 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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  • Dilution Calculator

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: ≥ 2.5 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.
  • 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.

    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).
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
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. 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
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Vadadustat Related Classifications

Help & FAQs
  • 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:

Vadadustat1000025-07-9PG-1016548 AKB-6548PG1016548PG 1016548AKB6548AKB 6548AKB-6548HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHErythropoiesis-stimulatingchronickidneydiseasenondialysis-dependentanemiaInhibitorinhibitorinhibit

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