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

Daprodustat  (Synonyms: GSK1278863)

Cat. No.: HY-17608 Purity: 99.80%
COA Handling Instructions

Molarity Calculator

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.

Daprodustat Chemical Structure

Daprodustat Chemical Structure

CAS No. : 960539-70-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 97 In-stock
Solution
10 mM * 1 mL in DMSO USD 97 In-stock
Solid
1 mg USD 35 In-stock
5 mg USD 88 In-stock
10 mg USD 140 In-stock
25 mg USD 230 In-stock
50 mg USD 400 In-stock
100 mg USD 660 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Daprodustat:

Daprodustat Related Antibodies

Top Publications Citing Use of Products

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

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HIF-1α HIF

  • 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.

Daprodustat Related Antibodies
Clinical Trial
Molecular Weight

393.43

Formula

C19H27N3O6
CAS No.
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 : 19.5 mg/mL (49.56 mM; Need ultrasonic and warming; 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
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)

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:  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)

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

Purity: 99.80%

COA (250 KB) HNMR (292 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
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, 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
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
15 mM 0.1694 mL 0.8472 mL 1.6945 mL 4.2362 mL
20 mM 0.1271 mL 0.6354 mL 1.2709 mL 3.1772 mL
25 mM 0.1017 mL 0.5083 mL 1.0167 mL 2.5417 mL
30 mM 0.0847 mL 0.4236 mL 0.8472 mL 2.1181 mL
40 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5886 mL
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Daprodustat 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:

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

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