2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. Glucocorticoid Receptor Cytochrome P450
  4. Dagrocorat

Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.

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

Dagrocorat Chemical Structure

Dagrocorat Chemical Structure

CAS No. : 1044535-52-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1241 In-stock
Solution
10 mM * 1 mL in DMSO USD 1306 In-stock
Solid
1 mg USD 545 In-stock
5 mg USD 1200 In-stock
10 mg USD 1800 In-stock
25 mg USD 3600 In-stock
50 mg USD 5750 In-stock
100 mg USD 9200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Dagrocorat:

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis[1].

IC50 & Target[1]

CYP3A

 

CYP2D6

 

In Vitro

Dagrocorat is metabolized by cytochrome P450 (CYP)3A to an N-oxide metabolite. Dagrocorat is a reversible inhibitor of several CYPs, such as CYP3A and CYP2D6[1].

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

494.55

Formula

C29H29F3N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@]1(C(F)(F)F)C[C@]2([H])[C@](C3=CC=C(C(NC(C=CC=N4)=C4C)=O)C=C3CC2)(CC1)CC5=CC=CC=C5
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 : 250 mg/mL (505.51 mM; Need ultrasonic; 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 2.0220 mL 10.1102 mL 20.2204 mL
5 mM 0.4044 mL 2.0220 mL 4.0441 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 6.25 mg/mL (12.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 6.25 mg/mL (12.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0220 mL 10.1102 mL 20.2204 mL 50.5510 mL
5 mM 0.4044 mL 2.0220 mL 4.0441 mL 10.1102 mL
10 mM 0.2022 mL 1.0110 mL 2.0220 mL 5.0551 mL
15 mM 0.1348 mL 0.6740 mL 1.3480 mL 3.3701 mL
20 mM 0.1011 mL 0.5055 mL 1.0110 mL 2.5276 mL
25 mM 0.0809 mL 0.4044 mL 0.8088 mL 2.0220 mL
30 mM 0.0674 mL 0.3370 mL 0.6740 mL 1.6850 mL
40 mM 0.0506 mL 0.2528 mL 0.5055 mL 1.2638 mL
50 mM 0.0404 mL 0.2022 mL 0.4044 mL 1.0110 mL
60 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8425 mL
80 mM 0.0253 mL 0.1264 mL 0.2528 mL 0.6319 mL
100 mM 0.0202 mL 0.1011 mL 0.2022 mL 0.5055 mL
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Dagrocorat Related Classifications

Help & FAQs
  • How should lyophilized recombinant proteins be reconstituted and stored?

    1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss. 2. Taking 10 μg as an example, first add 20 μL of reconstituted solution provided by MCE and use a pipette to gently resuspend the lyophilized protein until it is fully dissolved.. (For most proteins, the reconstitution solution we provide is sterile water. If a diluent other than water is required, it will be indicated in the product's Certificate of Analysis (COA).). 3. Add an additional 80 μL of buffer/culture medium containing carrier protein (either 0.1% BSA, 5% HSA, 10% FBS, or 5% trehalose), and then use a pipette to gently mix until uniform. The final concentration is should not be lower than 100 μg/mL. 4. Aliquot at least 20 μL per tube. 5. After aliquoting, store it frozen at a temperature ranging from -20ºC to -80ºC, and it can be preserved for 3 to 6 months.

  • How should solution-form recombinant proteins be stored?

    1. The product can be stored in its original form and diluted as needed upon use. 2. Alternatively, dilute with a buffer/culture medium containing a carrier protein (either 0.1% BSA, 5% HSA, 10% FBS, or 5% alginate), mix well by pipetting, and ensure that

  • Why is it necessary to add carrier proteins?

    Carrier proteins are commonly added to enhance the stability of recombinant proteins, preventing them from adhering to the walls of the container during freezing or thawing processes. Plastic tubes have a certain adsorptive capacity for proteins, which may lead to difficulty in separating the protein from the tube walls, resulting in a decrease in the actual concentration of the protein in the solution and thus affecting its activity. To minimize such losses, it is recommended to add a commonly used carrier protein solution prior to the long-term storage of recombinant protein products.

  • Carrier protein types and options?

    In cases where the carrier protein is not expected to influence the experimental outcomes, an appropriate carrier protein, such as 0.1% BSA (Bovine Serum Albumin), 5% HSA (Human Serum Albumin), 10% FBS (Fetal Bovine Serum), or 5% trehalose, can be incorpo

Keywords:

Dagrocorat1044535-52-5PF-00251802PF00251802PF 00251802Glucocorticoid ReceptorCytochrome P450CYPsglucocorticoidtime-dependentlivermicrosomesrheumatoidarthritisInhibitorinhibitorinhibit

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