2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. Difluprednate

Difluprednate  (Synonyms: ジフルプレドネート)

製品番号: HY-17569 純度: 99.64%
COA 取扱説明書 Technical Support

Difluprednate is a glucocorticoid receptor (GC receptor) agonist with a Ki of 0.78 nM. Difluprednate's active metabolite 21-deacetylated difluprednate (DFB) is a competitive agonist of GC receptors with a Ki of 0.061 nM. Difluprednate binds to GC receptors through metabolism to DFB, regulating the transcription of inflammatory mediator genes, thereby exerting anti-inflammatory activity. Difluprednate can be used for research related to ocular inflammation, such as postoperative inflammation, anterior uveitis, etc.

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Difluprednate 構造式

Difluprednate 構造式

CAS 番号 : 23674-86-4

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
50 mg USD 90 在庫あり
100 mg USD 144 在庫あり
500 mg USD 432 在庫あり
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Based on 1 publication(s) in Google Scholar

Other Forms of Difluprednate:

Difluprednate 関連抗体

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Phospholipase A PLD Phospholipase C

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製品説明

Difluprednate is a glucocorticoid receptor (GC receptor) agonist with a Ki of 0.78 nM. Difluprednate's active metabolite 21-deacetylated difluprednate (DFB) is a competitive agonist of GC receptors with a Ki of 0.061 nM. Difluprednate binds to GC receptors through metabolism to DFB, regulating the transcription of inflammatory mediator genes, thereby exerting anti-inflammatory activity. Difluprednate can be used for research related to ocular inflammation, such as postoperative inflammation, anterior uveitis, etc[1][2].

体内実験

Difluprednate (0.05% ophthalmic emulsion; ocular instillation; 5 times at 5-min intervals; single administration) is administered to the pigmented male rabbit model. Difluprednate can not be detected in the cornea, aqueous humor, iris/ciliary body 0.5 and 2 hours after instillation. Instead, Difluprednate is metabolized to 21-deacetylated difluprednate (DFB), 17-debutylated DFB (DF) and a new metabolite de-17-side chain-glucocorticoid metabolite (DF21C). The glucocorticoid receptor binding activity of DF21C (Ki=56 μM) is about 1000 times weaker than that of the parent drug[1].
Difluprednate (0.002%/0.01%/0.05% ophthalmic emulsion; ocular instillation; single administration; single dose) is metabolized to produce the active metabolite DFB in the male Japanese white rabbit model. The concentration of DFB in the aqueous humor and iris/ciliary body increases in a dose-dependent manner, and its glucocorticoid receptor binding activity (Ki=610 nM) is significantly stronger than that of the mother and other glucocorticoids[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

508.55

分子式

C27H34F2O7
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@]([C@]12C)(CC[C@@]1([H])[C@@](C[C@H](F)C3=CC4=O)([H])[C@@](F)([C@]3(C=C4)C)[C@@H](O)C2)OC(CCC)=O)COC(C)=O
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 (491.59 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 1.9664 mL 9.8319 mL 19.6637 mL
5 mM 0.3933 mL 1.9664 mL 3.9328 mL
10 mM 0.1966 mL 0.9832 mL 1.9664 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)

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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）

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体積 （開始）

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体積 （終了）

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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

純度: 99.64%

COA (253 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
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, 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 1.9664 mL 9.8319 mL 19.6638 mL 49.1594 mL
5 mM 0.3933 mL 1.9664 mL 3.9328 mL 9.8319 mL
10 mM 0.1966 mL 0.9832 mL 1.9664 mL 4.9159 mL
15 mM 0.1311 mL 0.6555 mL 1.3109 mL 3.2773 mL
20 mM 0.0983 mL 0.4916 mL 0.9832 mL 2.4580 mL
25 mM 0.0787 mL 0.3933 mL 0.7866 mL 1.9664 mL
30 mM 0.0655 mL 0.3277 mL 0.6555 mL 1.6386 mL
40 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2290 mL
50 mM 0.0393 mL 0.1966 mL 0.3933 mL 0.9832 mL
60 mM 0.0328 mL 0.1639 mL 0.3277 mL 0.8193 mL
80 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6145 mL
100 mM 0.0197 mL 0.0983 mL 0.1966 mL 0.4916 mL
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Difluprednate 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:

Difluprednate23674-86-4PhospholipaseInhibitorinhibitorinhibit

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