Daprodustat
Based on 20 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.91%
- No. CAS: 960539-70-2
- Fòrmula: C19H27N3O6
- Peso molecular:393.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-13426
RoxadustatHIF-PH Inhibitor -
HY-101277
VadadustatHIF PH Inhibitor -
HY-12654
MolidustatHypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor -
HY-15893
DMOGHIF-PH Inhibitor -
HY-109057
Enarodustat -
HY-103227
DesidustatHIF Hydroxylase Inhibitor -
HY-15468
IOX2HIF/HIF Prolyl-Hydroxylase Inhibitor -
HY-125840
BelzutifanHIF-2α Inhibitor -
HY-101023
MK-8617HIF PHD1-3 Inhibitor -
HY-15836
BAY 87-2243HIF-1 Inhibitor -
HY-15641
FG-2216HIF-PHD2 Inhibitor -
HY-120110
IOX4PHD2 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Daprodustat
More- Nat Commun. 2025 Jan 24;16(1):985. [Abstract]
- Acta Pharm Sin B. 2025 Mar;15(3):1497-1513. [Abstract]
- Phytomedicine. 2025 Mar:138:156392. [Abstract]
- Cell Rep. 2024 Jul 23;43(7):114471. [Abstract]
- Cell Rep. 2021 Apr 20;35(3):109020. [Abstract]
- J Med Chem. 2024 Mar 28;67(6):4525-4540. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Nov 29;1872(3):168124. [Abstract]
- iScience. 2023 Nov 9;26(12):108424. [Abstract]
- Anal Bioanal Chem. 2022 Nov;414(28):8125-8142. [Abstract]
- J Biol Chem. 2021 Jan-Jun:296:100397. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- Sep Sci Plus. 2025 Apr 14.
- J Anal Toxicol. 2021 Feb 13;45(2):184-194. [Abstract]
- Drug Test Anal. 2021 Feb;13(2):283-298. [Abstract]
- ChemistrySelect. 2025 Mar 31.
- bioRxiv. 2025 Aug 12.
- Patent. US20250262229A1.
- bioRxiv. 2023 Nov 2.
- SSRN. 2023 Aug 15.
- bioRxiv. 2023 Feb 12.
Customer Validation & Images
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WB
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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IF
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Bio/Physico-chemical Assay
Actividad biológica
Descripciòn
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. .
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 960539-70-2
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Appearance Solid
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Peso molecular 393.43
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Fòrmula C19H27N3O6
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Color White to off-white
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SMILES
O=C(O)CNC(C(C(N1C2CCCCC2)=O)C(N(C3CCCCC3)C1=O)=O)=O
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Synonyms
GSK1278863
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (20)
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Journal Impact Factor
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Most Recent
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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
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.
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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
Daprodustat purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Mar;15(3):1497-1513. [Abstract]
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. [Abstract]
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.
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Phytomedicine
Polydatin mitigates thrombosis by inhibiting PHD2-induced proline hydroxylation on collagen, reducing platelet adhesion. [Abstract]2025 Mar:138:156392. PMID: 39826283 -
Cell Rep
2024 Jul 23;43(7):114471. PMID: 38996069 -
Cell Rep
Hypoxic and pharmacological activation of HIF inhibits SARS-CoV-2 infection of lung epithelial cells. [Abstract]2021 Apr 20;35(3):109020. PMID: 33852916
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.
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J Med Chem
Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate. [Abstract]2024 Mar 28;67(6):4525-4540. PMID: 38294854 -
Biochim Biophys Acta Mol Basis Dis
Prolyl-hydroxylase domain inhibition enhances collagen levels in oral mucosa-derived fibroblasts. [Abstract]2025 Nov 29;1872(3):168124. PMID: 41319981 -
iScience
The hypoxia-inducible factor EPAS1 is required for spermatogonial stem cell function in regenerative conditions. [Abstract]2023 Nov 9;26(12):108424. PMID: 38077147
Daprodustat purchased from MedChemExpress. Usage Cited in: iScience. 2023 Nov 9;26(12):108424. [Abstract]
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. [Abstract]
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. [Abstract]
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. [Abstract]
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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Anal Bioanal Chem
Generic approach for the discovery of drug metabolites in horses based on data-dependent acquisition by liquid chromatography high-resolution mass spectrometry and its applications to pharmacokinetic study of daprodustat. [Abstract]2022 Nov;414(28):8125-8142. PMID: 36181513 -
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 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
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J Anal Toxicol
2021 Feb 13;45(2):184-194. PMID: 32435795 -
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 -
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Solvente y solubilidad
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)
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.
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.
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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
HY-17608 Related Classifications
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