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Daprodustat (GSK1278863)

Catalog No.S8171 Purity:99.71%

Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.

Daprodustat (GSK1278863) Chemical Structure

CAS No. 960539-70-2

Purity & Quality Control

Batch: Purity: 99.71%

99.71

Daprodustat (GSK1278863) Related Products

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Signaling Pathway

HIF Signaling Pathway

Biological Activity

Description

Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.

Targets

HIF-PH ^[1]

In vitro
In vitro	GSK1278863 induces an effective EPO response and stimulates non-EPO mechanisms for erythropoiesis. ^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05682326	Recruiting	Anaemia	GlaxoSmithKline	September 6 2023	Phase 3
NCT05951192	Active not recruiting	Anemia\|Renal Insufficiency Chronic\|Renal Anemia	USRC Kidney Research\|GlaxoSmithKline	July 1 2023	Phase 4
NCT04640311	Completed	Anaemia	GlaxoSmithKline	December 18 2020	Phase 1

References
[1] Brigandi RA, et al. Am J Kidney Dis. 2016. doi: 10.1053/j.ajkd.2015.11.021.

References

[1] Brigandi RA, et al. Am J Kidney Dis. 2016. doi: 10.1053/j.ajkd.2015.11.021.

Chemical Information & Solubility

Molecular Weight	393.43	Formula	C₁₉H₂₇N₃O₆
CAS No.	960539-70-2	SDF	Download Daprodustat (GSK1278863) SDF
Smiles	C1CCC(CC1)N2C(=O)C(C(=O)N(C2=O)C3CCCCC3)C(=O)NCC(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 5 mg/mL ( (12.7 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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