2. Metabolic Enzyme/Protease Apoptosis
  3. Phospholipase Apoptosis
  4. Darapladib

Darapladib  (Synonyms: SB-480848)

製品番号: HY-10521 純度: 99.94%
COA 取扱説明書

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Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer.

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Darapladib 構造式

Darapladib 構造式

CAS 番号 : 356057-34-6

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
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 191 在庫あり
Solution
10 mM * 1 mL in DMSO USD 191 在庫あり
Solid
5 mg USD 130 在庫あり
10 mg USD 210 在庫あり
25 mg USD 420 在庫あり
50 mg USD 680 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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Based on 5 publication(s) in Google Scholar

Darapladib 関連抗体

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製品説明

Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer[1][2][3][4].

IC50 & Target

IC50: 0.25 nM (Lp-PLA2)[1]
体外実験

Darapladib (5 μM; 6, 12 h) induces cell cycle arrest in glioma cells (C6 glioma cells and U251MG cells)[2].
Darapladib (5 μM; 3, 6 h) triggers cell apoptosis in glioma cells[2].
Darapladib (5 μM; 5, 15, 30, 60 and 90 min) induces an increase in phosphorylation of ERK1/2 proteins in glioma cells[2].

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

Darapladib 関連抗体

Apoptosis Analysis[2]

Cell Line: C6 glioma cells and U251MG cells.
Concentration: 5 μM
Incubation Time: 3, 6 h
Result: Triggered cell apoptosis in glioma cells.

Cell Cycle Analysis[2]

Cell Line: C6 glioma cells and U251MG cells.
Concentration: 5 μM
Incubation Time: 6, 12 h
Result: Induced cell cycle arrest in glioma cells.

Western Blot Analysis[2]

Cell Line: C6 glioma cells and U251MG cells.
Concentration: 5 μM
Incubation Time: 5, 15, 30, 60 and 90 min
Result: Induced an increase in phosphorylation of ERK1/2 proteins, but reduced AKT phosphorylation in glioma cells.
体内実験

Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) significantly inhibits serum Lp-PLA2 activity in LDLR-deficient mice[3].
Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) decreases serum hs-CRP and IL-6 levels[3].

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

Animal Model: Male homozygous LDLR-deficient mice (C57/Bl6 genetic background)[3].
Dosage: 50 mg/kg
Administration: Oral administration; once daily for 6 weeks.
Result: Significantly inhibited activity of serum Lp-PLA2.
臨床実験
分子量

666.77

分子式

C36H38F4N4O2S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=C(CSC(N(CC(N(CCN(CC)CC)CC2=CC=C(C3=CC=C(C(F)(F)F)C=C3)C=C2)=O)C4=C5CCC4)=NC5=O)C=C1
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 : ≥ 100 mg/mL (149.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4998 mL 7.4988 mL 14.9977 mL
5 mM 0.3000 mL 1.4998 mL 2.9995 mL
10 mM 0.1500 mL 0.7499 mL 1.4998 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

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: ≥ 2.5 mg/mL (3.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (3.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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.
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

純度: 99.94%

COA (248 KB) HNMR (283 KB) LCMS (265 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 1.4998 mL 7.4988 mL 14.9977 mL 37.4942 mL
5 mM 0.3000 mL 1.4998 mL 2.9995 mL 7.4988 mL
10 mM 0.1500 mL 0.7499 mL 1.4998 mL 3.7494 mL
15 mM 0.1000 mL 0.4999 mL 0.9998 mL 2.4996 mL
20 mM 0.0750 mL 0.3749 mL 0.7499 mL 1.8747 mL
25 mM 0.0600 mL 0.3000 mL 0.5999 mL 1.4998 mL
30 mM 0.0500 mL 0.2500 mL 0.4999 mL 1.2498 mL
40 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9374 mL
50 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7499 mL
60 mM 0.0250 mL 0.1250 mL 0.2500 mL 0.6249 mL
80 mM 0.0187 mL 0.0937 mL 0.1875 mL 0.4687 mL
100 mM 0.0150 mL 0.0750 mL 0.1500 mL 0.3749 mL
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Darapladib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

Darapladib356057-34-6SB-480848SB480848SB 480848PhospholipaseApoptosisatherosclerosiscancerglioma cellapoptosisU251MG cellssubG1 cellcycle arrestInhibitorinhibitorinhibit

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