Daprodustat (Synonyms: GSK1278863)

Name: Daprodustat
Brand: MedChemExpress
SKU: HY-17608
Rating: 5.0 (20 reviews)

Cat. No.: HY-17608 Purity: 99.91%: Data Sheet
COA

SDS
Handling Instructions
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Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.

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

CAS No. : 960539-70-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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 20 publication(s) in Google Scholar

Other Forms of Daprodustat:

Daprodustat (Standard) Get quote

20 Publications Citing Use of MCE Daprodustat

In Vivo Efficacy Study

Bio/Physico-chemical Assay

Cell Proliferation/Viability Assay

: Daprodustat 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 + Daprodustat (GSK1278863) (250uM), Roxadustat, Vadadustat, or Daprodustat (GSK1278863) (250uM). All treatments were for 24 h. n = 3–6.

: Daprodustat purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Mar;15(3):1497-1513.; The measurements of thrombus wet weight indicate that ASP, CK and Daprodustat (Dap), whether administered alone or in combination, exhibited sound antithrombotic effects. Furthermore, the combined use of ASP and CK displayed superior efficacy compared to their individual use, and similar effects were observed with the combination of Dap and ASP. SD rats (200–220 g) were randomly divided into seven groups: control (ctrl), model (mod), ASP (10 mg/kg), CK (20 mg/kg), Dap (10 mg/kg), ASP + CK (5 + 10 mg/kg), and ASP + Dap (5 + 5 mg/kg) groups. Continuous intraperitoneal administration of drugs was performed for 14 days. Anesthesia was induced in rats 1 h after the final administration, and blunt dissection to isolate the carotid artery.

: Daprodustat purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Mar;15(3):1497-1513.; The measurements of thrombus length indicate that ASP, CK and Daprodustat (Dap), whether administered alone or in combination, exhibited sound antithrombotic effects. Furthermore, the combined use of ASP and CK displayed superior efficacy compared to their individual use, and similar effects were observed with the combination of Dap and ASP. SD rats (200–220 g) were randomly divided into seven groups: control (ctrl), model (mod), ASP (10 mg/kg), CK (20 mg/kg), Dap (10 mg/kg), ASP + CK (5 + 10 mg/kg), and ASP + Dap (5 + 5 mg/kg) groups. Continuous intraperitoneal administration of drugs was performed for 14 days. Anesthesia was induced in rats 1 h after the final administration, and blunt dissection to isolate the carotid artery.

: Daprodustat purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Apr 20;35(3):109020. [Abstract]; Calu-3 cells were treated with increasing concentrations of Daprodustat (GSK: 1278863, 0-50 μM), Molidustat (Bay 85-3934), and Roxadustat (FG-4592) and were infected with SARS-CoV-2, and viral replication was assessed 24 h later. Data are expressed relative to UT cells.

: Daprodustat purchased from MedChemExpress. Usage Cited in: iScience. 2023 Nov 9;26(12):108424.; Immunofluorescence images depicting increased EPAS1 expression (red) in undifferentiated spermatogonia from culture following 24 h exposure to 250 μM Daprodustat, as compared to a vehicle (DMSO) control.

: Daprodustat purchased from MedChemExpress. Usage Cited in: iScience. 2023 Nov 9;26(12):108424.; Quantification of corrected total cell fluorescence (CTCF) of EPAS1 expression comparing undifferentiated spermatogonia from culture following 24 h exposure to 250 μM Daprodustat, as compared to a vehicle (DMSO) control.

: Daprodustat purchased from MedChemExpress. Usage Cited in: iScience. 2023 Nov 9;26(12):108424.; Cell viability (Live/dead flow cytometry assay) of undifferentiated spermatogonia from culture following 24 h exposure to 250 μM Daprodustat or vehicle (DMSO control).

: Daprodustat purchased from MedChemExpress. Usage Cited in: iScience. 2023 Nov 9;26(12):108424.; Bulk RNA-seq analysis comparing undifferentiated spermatogonia from culture treated with either DMSO or 250 M Daprodustat. Downregulated genes denoted by purple circles and upregulated genes denoted by yellow circles had a false discovery rate (FDR) of p < 0.05.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.

In Vitro

GSK1278863 is an orally administered small-molecule PHI, and stimulates endogenous EPO synthesis and induce effective erythropoiesis^[1].
GSK1278863 has been shown to increase erythropoietin levels, leading to increases in hemoglobin, hematocrit and red blood cell numbers^[2].

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

Clinical Trial

Molecular Weight

393.43

Formula

C₁₉H₂₇N₃O₆

CAS No.

960539-70-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CNC(C(C(N1C2CCCCC2)=O)C(N(C3CCCCC3)C1=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (12.71 mM; ultrasonic and warming and heat to 60°C; 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	2.5417 mL	12.7087 mL	25.4175 mL
5 mM	0.5083 mL	2.5417 mL	5.0835 mL
10 mM	0.2542 mL	1.2709 mL	2.5417 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (12.71 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.91%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (250 KB) HNMR (293 KB) RP-HPLC (246 KB) MS (71 KB)

Handling Instructions (2659 KB)

References

[1]. Brigandi RA, et al. A Novel Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor (GSK1278863) for Anemia in CKD: A 28-Day, Phase 2A Randomized Trial. Am J Kidney Dis. 2016 Jun;67(6):861-71 [Content Brief]

[2]. Hara K, et al. Pharmacokinetics, pharmacodynamics and safety of single, oral doses of GSK1278863, a novel HIF-prolyl hydroxylase inhibitor, in healthy Japanese and Caucasian subjects. Drug Metab Pharmacokinet. 2015 Dec;30(6):410-8 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5417 mL	12.7087 mL	25.4175 mL	63.5437 mL
	5 mM	0.5083 mL	2.5417 mL	5.0835 mL	12.7087 mL
	10 mM	0.2542 mL	1.2709 mL	2.5417 mL	6.3544 mL

Daprodustat Related Classifications

Cardiovascular Disease

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:

Daprodustat960539-70-2GSK1278863GSK 1278863GSK-1278863HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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Daprodustat (Synonyms: GSK1278863)

Customer Review

Other Forms of Daprodustat:

Daprodustat Related Antibodies

20 Publications Citing Use of MCE Daprodustat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Daprodustat Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Daprodustat Related Classifications

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Customer Review

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