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

Dagrocorat  (Synonyms: PF-00251802)

製品番号: HY-16718 純度: 99.90%
COA 取扱説明書 Technical Support

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.

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Dagrocorat

Dagrocorat 構造式

CAS 番号 : 1044535-52-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 925 在庫あり
Solution
10 mM * 1 mL in DMSO USD 925 在庫あり
Solid
1 mg $545 在庫あり
5 mg $850 在庫あり
10 mg $1400 在庫あり
25 mg $2800 在庫あり
50 mg $4500 在庫あり
100 mg $7300 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Other Forms of Dagrocorat:

Dagrocorat 関連抗体

Top Publications Citing Use of Products

Cytochrome P450 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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製品説明

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

 

体外実験

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.

Dagrocorat 関連抗体
分子量

494.55

分子式

C29H29F3N2O2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.2022 mL 1.0110 mL 2.0220 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)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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, . 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.
純度とドキュメンテーション
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

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

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製品名:
Dagrocorat
製品番号:
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