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

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

Cat. No.: HY-101277 Purity: 99.63%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 118 In-stock
Estimated Time of Arrival: December 31
2 mg USD 70 In-stock
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5 mg USD 120 In-stock
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10 mg USD 190 In-stock
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50 mg USD 490 In-stock
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100 mg USD 690 In-stock
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Based on 2 publication(s) in Google Scholar

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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].

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

Clinical Trial
Molecular Weight

306.70

Formula

C₁₄H₁₁ClN₂O₄

CAS No.

1000025-07-9

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)

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
10 mM 0.3261 mL 1.6303 mL 3.2605 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

VadadustatPG-1016548 AKB-6548PG1016548PG 1016548AKB6548AKB 6548AKB-6548HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHErythropoiesis-stimulatingchronickidneydiseasenondialysis-dependentanemiaInhibitorinhibitorinhibit

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Vadadustat
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